연구용
Tozasertib (VX-680) Aurora Kinase 억제제
제품 번호S1048
화학 구조
분자량: 464.59
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품질 관리
배치:
순도:
99.99%
99.99
세포 배양, 처리 및 작업 농도
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| BE-13 | Growth Inhibition Assay | IC50=0.00338 μM | SANGRER | |||
| RS4-11 | Growth Inhibition Assay | IC50=0.00404 μM | SANGRER | |||
| MFH-ino | Growth Inhibition Assay | IC50=0.0099 μM | SANGRER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=0.01434 μM | SANGRER | |||
| 697 | Growth Inhibition Assay | IC50=0.02471 μM | SANGRER | |||
| NALM-6 | Growth Inhibition Assay | IC50=0.02552 μM | SANGRER | |||
| ES8 | Growth Inhibition Assay | IC50=0.04613 μM | SANGRER | |||
| HUTU-80 | Growth Inhibition Assay | IC50=0.05299 μM | SANGRER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=0.07782 μM | SANGRER | |||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=0.07879 μM | SANGRER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=0.08789 μM | SANGRER | |||
| BL-41 | Growth Inhibition Assay | IC50=0.10445 μM | SANGRER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=0.11563 μM | SANGRER | |||
| SW954 | Growth Inhibition Assay | IC50=0.12229 μM | SANGRER | |||
| BV-173 | Growth Inhibition Assay | IC50=0.12641 μM | SANGRER | |||
| TE-11 | Growth Inhibition Assay | IC50=0.14982 μM | SANGRER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=0.15965 μM | SANGRER | |||
| SIG-M5 | Growth Inhibition Assay | IC50=0.16707 μM | SANGRER | |||
| OCUB-M | Growth Inhibition Assay | IC50=0.16983 μM | SANGRER | |||
| K052 | Growth Inhibition Assay | IC50=0.1948 μM | SANGRER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=0.20086 μM | SANGRER | |||
| SW982 | Growth Inhibition Assay | IC50=0.2138 μM | SANGRER | |||
| LB647-SCLC | Growth Inhibition Assay | IC50=0.21523 μM | SANGRER | |||
| PSN1 | Growth Inhibition Assay | IC50=0.22026 μM | SANGRER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=0.22591 μM | SANGRER | |||
| ST486 | Growth Inhibition Assay | IC50=0.23087 μM | SANGRER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=0.23337 μM | SANGRER | |||
| EW-16 | Growth Inhibition Assay | IC50=0.23768 μM | SANGRER | |||
| KS-1 | Growth Inhibition Assay | IC50=0.23785 μM | SANGRER | |||
| SR | Growth Inhibition Assay | IC50=0.24564 μM | SANGRER | |||
| KM12 | Growth Inhibition Assay | IC50=0.2636 μM | SANGRER | |||
| EM-2 | Growth Inhibition Assay | IC50=0.26641 μM | SANGRER | |||
| MEG-01 | Growth Inhibition Assay | IC50=0.27849 μM | SANGRER | |||
| NB13 | Growth Inhibition Assay | IC50=0.27984 μM | SANGRER | |||
| RKO | Growth Inhibition Assay | IC50=0.30813 μM | SANGRER | |||
| CESS | Growth Inhibition Assay | IC50=0.31328 μM | SANGRER | |||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.33459 μM | SANGRER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=0.33781 μM | SANGRER | |||
| A388 | Growth Inhibition Assay | IC50=0.34086 μM | SANGRER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=0.35178 μM | SANGRER | |||
| IMR-5 | Growth Inhibition Assay | IC50=0.3554 μM | SANGRER | |||
| KARPAS-422 | Growth Inhibition Assay | IC50=0.37272 μM | SANGRER | |||
| MRK-nu-1 | Growth Inhibition Assay | IC50=0.3813 μM | SANGRER | |||
| BL-70 | Growth Inhibition Assay | IC50=0.38974 μM | SANGRER | |||
| LXF-289 | Growth Inhibition Assay | IC50=0.40406 μM | SANGRER | |||
| RL95-2 | Growth Inhibition Assay | IC50=0.40567 μM | SANGRER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=0.42676 μM | SANGRER | |||
| K-562 | Growth Inhibition Assay | IC50=0.43472 μM | SANGRER | |||
| NCI-H510A | Growth Inhibition Assay | IC50=0.43823 μM | SANGRER | |||
| NCI-H524 | Growth Inhibition Assay | IC50=0.51147 μM | SANGRER | |||
| KE-37 | Growth Inhibition Assay | IC50=0.52102 μM | SANGRER | |||
| KP-N-YS | Growth Inhibition Assay | IC50=0.54392 μM | SANGRER | |||
| LS-411N | Growth Inhibition Assay | IC50=0.57752 μM | SANGRER | |||
| CTV-1 | Growth Inhibition Assay | IC50=0.58773 μM | SANGRER | |||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=0.63571 μM | SANGRER | |||
| HT-144 | Growth Inhibition Assay | IC50=0.63798 μM | SANGRER | |||
| NCI-H187 | Growth Inhibition Assay | IC50=0.6413 μM | SANGRER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=0.64403 μM | SANGRER | |||
| CCRF-CEM | Growth Inhibition Assay | IC50=0.65346 μM | SANGRER | |||
| ONS-76 | Growth Inhibition Assay | IC50=0.66458 μM | SANGRER | |||
| IST-SL2 | Growth Inhibition Assay | IC50=0.71982 μM | SANGRER | |||
| NB6 | Growth Inhibition Assay | IC50=0.77254 μM | SANGRER | |||
| SK-PN-DW | Growth Inhibition Assay | IC50=0.7914 μM | SANGRER | |||
| HCC1599 | Growth Inhibition Assay | IC50=0.80874 μM | SANGRER | |||
| MC116 | Growth Inhibition Assay | IC50=0.85011 μM | SANGRER | |||
| TE-15 | Growth Inhibition Assay | IC50=0.85098 μM | SANGRER | |||
| HOP-62 | Growth Inhibition Assay | IC50=0.86329 μM | SANGRER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=0.86385 μM | SANGRER | |||
| HCE-4 | Growth Inhibition Assay | IC50=0.88063 μM | SANGRER | |||
| ALL-PO | Growth Inhibition Assay | IC50=0.88175 μM | SANGRER | |||
| KGN | Growth Inhibition Assay | IC50=0.89995 μM | SANGRER | |||
| ML-2 | Growth Inhibition Assay | IC50=0.90259 μM | SANGRER | |||
| ES4 | Growth Inhibition Assay | IC50=0.91128 μM | SANGRER | |||
| SF126 | Growth Inhibition Assay | IC50=0.94819 μM | SANGRER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=0.96189 μM | SANGRER | |||
| HCC1187 | Growth Inhibition Assay | IC50=1.00505 μM | SANGRER | |||
| DU-4475 | Growth Inhibition Assay | IC50=1.01756 μM | SANGRER | |||
| NKM-1 | Growth Inhibition Assay | IC50=1.02775 μM | SANGRER | |||
| HL-60 | Growth Inhibition Assay | IC50=1.06574 μM | SANGRER | |||
| SBC-1 | Growth Inhibition Assay | IC50=1.12542 μM | SANGRER | |||
| TE-10 | Growth Inhibition Assay | IC50=1.12946 μM | SANGRER | |||
| ETK-1 | Growth Inhibition Assay | IC50=1.13613 μM | SANGRER | |||
| HAL-01 | Growth Inhibition Assay | IC50=1.16709 μM | SANGRER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=1.18005 μM | SANGRER | |||
| EW-1 | Growth Inhibition Assay | IC50=1.18562 μM | SANGRER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=1.21111 μM | SANGRER | |||
| SK-LMS-1 | Growth Inhibition Assay | IC50=1.22212 μM | SANGRER | |||
| DEL | Growth Inhibition Assay | IC50=1.25643 μM | SANGRER | |||
| GT3TKB | Growth Inhibition Assay | IC50=1.28057 μM | SANGRER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=1.35405 μM | SANGRER | |||
| CMK | Growth Inhibition Assay | IC50=1.42117 μM | SANGRER | |||
| NB5 | Growth Inhibition Assay | IC50=1.64229 μM | SANGRER | |||
| NCI-H1963 | Growth Inhibition Assay | IC50=1.70583 μM | SANGRER | |||
| KURAMOCHI | Growth Inhibition Assay | IC50=1.78911 μM | SANGRER | |||
| TE-8 | Growth Inhibition Assay | IC50=1.80368 μM | SANGRER | |||
| NCI-H1304 | Growth Inhibition Assay | IC50=1.83073 μM | SANGRER | |||
| A101D | Growth Inhibition Assay | IC50=1.87395 μM | SANGRER | |||
| SCLC-21H | Growth Inhibition Assay | IC50=1.97057 μM | SANGRER | |||
| GB-1 | Growth Inhibition Assay | IC50=2.01647 μM | SANGRER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=2.02654 μM | SANGRER | |||
| ATN-1 | Growth Inhibition Assay | IC50=2.02858 μM | SANGRER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=2.06244 μM | SANGRER | |||
| RPMI-6666 | Growth Inhibition Assay | IC50=2.16207 μM | SANGRER | |||
| NB17 | Growth Inhibition Assay | IC50=2.2927 μM | SANGRER | |||
| IST-SL1 | Growth Inhibition Assay | IC50=2.29765 μM | SANGRER | |||
| SH-4 | Growth Inhibition Assay | IC50=2.32469 μM | SANGRER | |||
| K5 | Growth Inhibition Assay | IC50=2.40319 μM | SANGRER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=2.4613 μM | SANGRER | |||
| ACN | Growth Inhibition Assay | IC50=2.50213 μM | SANGRER | |||
| TGW | Growth Inhibition Assay | IC50=2.65832 μM | SANGRER | |||
| NCI-H2107 | Growth Inhibition Assay | IC50=2.83711 μM | SANGRER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=2.83838 μM | SANGRER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=2.86868 μM | SANGRER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=2.88126 μM | SANGRER | |||
| LU-134-A | Growth Inhibition Assay | IC50=2.8926 μM | SANGRER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=2.91253 μM | SANGRER | |||
| NOMO-1 | Growth Inhibition Assay | IC50=3.02274 μM | SANGRER | |||
| RH-1 | Growth Inhibition Assay | IC50=3.17291 μM | SANGRER | |||
| LOUCY | Growth Inhibition Assay | IC50=3.18693 μM | SANGRER | |||
| TE-9 | Growth Inhibition Assay | IC50=3.26736 μM | SANGRER | |||
| PF-382 | Growth Inhibition Assay | IC50=3.35778 μM | SANGRER | |||
| RPMI-8402 | Growth Inhibition Assay | IC50=3.58603 μM | SANGRER | |||
| HEL | Growth Inhibition Assay | IC50=3.632 μM | SANGRER | |||
| NOS-1 | Growth Inhibition Assay | IC50=3.84754 μM | SANGRER | |||
| ES1 | Growth Inhibition Assay | IC50=3.92293 μM | SANGRER | |||
| NCI-H2171 | Growth Inhibition Assay | IC50=3.92423 μM | SANGRER | |||
| NCI-H747 | Growth Inhibition Assay | IC50=3.94221 μM | SANGRER | |||
| MHH-NB-11 | Growth Inhibition Assay | IC50=3.95312 μM | SANGRER | |||
| MZ1-PC | Growth Inhibition Assay | IC50=3.9924 μM | SANGRER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=4.02467 μM | SANGRER | |||
| NMC-G1 | Growth Inhibition Assay | IC50=4.22723 μM | SANGRER | |||
| SW872 | Growth Inhibition Assay | IC50=4.3434 μM | SANGRER | |||
| TE-12 | Growth Inhibition Assay | IC50=4.56394 μM | SANGRER | |||
| LU-139 | Growth Inhibition Assay | IC50=4.61835 μM | SANGRER | |||
| HC-1 | Growth Inhibition Assay | IC50=4.69494 μM | SANGRER | |||
| COR-L279 | Growth Inhibition Assay | IC50=4.75891 μM | SANGRER | |||
| SF268 | Growth Inhibition Assay | IC50=4.79916 μM | SANGRER | |||
| MC-CAR | Growth Inhibition Assay | IC50=5.06757 μM | SANGRER | |||
| TK10 | Growth Inhibition Assay | IC50=5.35469 μM | SANGRER | |||
| TE-1 | Growth Inhibition Assay | IC50=5.49004 μM | SANGRER | |||
| NCI-H2126 | Growth Inhibition Assay | IC50=5.64574 μM | SANGRER | |||
| Daudi | Growth Inhibition Assay | IC50=5.6912 μM | SANGRER | |||
| NCI-H1648 | Growth Inhibition Assay | IC50=5.81454 μM | SANGRER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=5.98597 μM | SANGRER | |||
| DJM-1 | Growth Inhibition Assay | IC50=6.34666 μM | SANGRER | |||
| LS-1034 | Growth Inhibition Assay | IC50=6.7566 μM | SANGRER | |||
| NCI-H1581 | Growth Inhibition Assay | IC50=6.78405 μM | SANGRER | |||
| UACC-257 | Growth Inhibition Assay | IC50=7.04512 μM | SANGRER | |||
| KM-H2 | Growth Inhibition Assay | IC50=7.18457 μM | SANGRER | |||
| NCI-H1436 | Growth Inhibition Assay | IC50=7.69932 μM | SANGRER | |||
| IA-LM | Growth Inhibition Assay | IC50=7.859 μM | SANGRER | |||
| NCI-H526 | Growth Inhibition Assay | IC50=8.25637 μM | SANGRER | |||
| GCIY | Growth Inhibition Assay | IC50=8.36965 μM | SANGRER | |||
| CP67-MEL | Growth Inhibition Assay | IC50=8.5326 μM | SANGRER | |||
| KALS-1 | Growth Inhibition Assay | IC50=8.83851 μM | SANGRER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=8.90265 μM | SANGRER | |||
| 8-MG-BA | Growth Inhibition Assay | IC50=9.32844 μM | SANGRER | |||
| KY821 | Growth Inhibition Assay | IC50=9.77484 μM | SANGRER | |||
| SNB75 | Growth Inhibition Assay | IC50=10.076 μM | SANGRER | |||
| NCCIT | Growth Inhibition Assay | IC50=11.0582 μM | SANGRER | |||
| SJSA-1 | Growth Inhibition Assay | IC50=11.2891 μM | SANGRER | |||
| LB373-MEL-D | Growth Inhibition Assay | IC50=11.3827 μM | SANGRER | |||
| TALL-1 | Growth Inhibition Assay | IC50=11.4058 μM | SANGRER | |||
| NB69 | Growth Inhibition Assay | IC50=11.7705 μM | SANGRER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=11.9426 μM | SANGRER | |||
| DMS-153 | Growth Inhibition Assay | IC50=12.0426 μM | SANGRER | |||
| OPM-2 | Growth Inhibition Assay | IC50=12.1596 μM | SANGRER | |||
| NB1 | Growth Inhibition Assay | IC50=12.29 μM | SANGRER | |||
| A3-KAW | Growth Inhibition Assay | IC50=12.3236 μM | SANGRER | |||
| NCI-H1882 | Growth Inhibition Assay | IC50=12.4066 μM | SANGRER | |||
| KG-1 | Growth Inhibition Assay | IC50=12.6545 μM | SANGRER | |||
| LC4-1 | Growth Inhibition Assay | IC50=12.7706 μM | SANGRER | |||
| HCE-T | Growth Inhibition Assay | IC50=13.0049 μM | SANGRER | |||
| NEC8 | Growth Inhibition Assay | IC50=13.1038 μM | SANGRER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=13.5788 μM | SANGRER | |||
| EW-3 | Growth Inhibition Assay | IC50=13.7402 μM | SANGRER | |||
| CTB-1 | Growth Inhibition Assay | IC50=14.0329 μM | SANGRER | |||
| LS-123 | Growth Inhibition Assay | IC50=14.1588 μM | SANGRER | |||
| NCI-H1417 | Growth Inhibition Assay | IC50=14.3052 μM | SANGRER | |||
| MZ7-mel | Growth Inhibition Assay | IC50=14.4433 μM | SANGRER | |||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=15.6326 μM | SANGRER | |||
| ES6 | Growth Inhibition Assay | IC50=16.2361 μM | SANGRER | |||
| HH | Growth Inhibition Assay | IC50=17.1963 μM | SANGRER | |||
| SF539 | Growth Inhibition Assay | IC50=17.9922 μM | SANGRER | |||
| Calu-6 | Growth Inhibition Assay | IC50=19.239 μM | SANGRER | |||
| SK-MM-2 | Growth Inhibition Assay | IC50=19.555 μM | SANGRER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=19.6663 μM | SANGRER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=19.8227 μM | SANGRER | |||
| CAL-148 | Growth Inhibition Assay | IC50=20.9934 μM | SANGRER | |||
| EVSA-T | Growth Inhibition Assay | IC50=21.1499 μM | SANGRER | |||
| LP-1 | Growth Inhibition Assay | IC50=21.3432 μM | SANGRER | |||
| BOKU | Growth Inhibition Assay | IC50=21.4533 μM | SANGRER | |||
| KLE | Growth Inhibition Assay | IC50=22.1903 μM | SANGRER | |||
| LB831-BLC | Growth Inhibition Assay | IC50=25.1526 μM | SANGRER | |||
| NCI-H889 | Growth Inhibition Assay | IC50=25.1931 μM | SANGRER | |||
| REH | Growth Inhibition Assay | IC50=25.4671 μM | SANGRER | |||
| KP-N-RT-BM-1 | Growth Inhibition Assay | IC50=25.4752 μM | SANGRER | |||
| MPP-89 | Growth Inhibition Assay | IC50=25.5314 μM | SANGRER | |||
| no-11 | Growth Inhibition Assay | IC50=25.747 μM | SANGRER | |||
| NCI-H748 | Growth Inhibition Assay | IC50=25.7627 μM | SANGRER | |||
| LB2518-MEL | Growth Inhibition Assay | IC50=27.1773 μM | SANGRER | |||
| TGBC1TKB | Growth Inhibition Assay | IC50=27.5585 μM | SANGRER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=28.0734 μM | SANGRER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=28.6143 μM | SANGRER | |||
| U-266 | Growth Inhibition Assay | IC50=28.6366 μM | SANGRER | |||
| SNU-C1 | Growth Inhibition Assay | IC50=28.943 μM | SANGRER | |||
| SW962 | Growth Inhibition Assay | IC50=30.2747 μM | SANGRER | |||
| Raji | Growth Inhibition Assay | IC50=30.5592 μM | SANGRER | |||
| KNS-42 | Growth Inhibition Assay | IC50=30.8956 μM | SANGRER | |||
| LB996-RCC | Growth Inhibition Assay | IC50=31.1702 μM | SANGRER | |||
| CHP-126 | Growth Inhibition Assay | IC50=31.1984 μM | SANGRER | |||
| RXF393 | Growth Inhibition Assay | IC50=32.497 μM | SANGRER | |||
| COLO-684 | Growth Inhibition Assay | IC50=32.6438 μM | SANGRER | |||
| A704 | Growth Inhibition Assay | IC50=33.5538 μM | SANGRER | |||
| A253 | Growth Inhibition Assay | IC50=33.5852 μM | SANGRER | |||
| KNS-81-FD | Growth Inhibition Assay | IC50=34.5456 μM | SANGRER | |||
| TE-441-T | Growth Inhibition Assay | IC50=34.6371 μM | SANGRER | |||
| HCC2157 | Growth Inhibition Assay | IC50=35.4619 μM | SANGRER | |||
| ES3 | Growth Inhibition Assay | IC50=36.675 μM | SANGRER | |||
| NCI-H1155 | Growth Inhibition Assay | IC50=37.815 μM | SANGRER | |||
| SNU-C2B | Growth Inhibition Assay | IC50=38.1654 μM | SANGRER | |||
| JAR | Growth Inhibition Assay | IC50=38.2449 μM | SANGRER | |||
| GDM-1 | Growth Inhibition Assay | IC50=38.9116 μM | SANGRER | |||
| KU812 | Growth Inhibition Assay | IC50=41.507 μM | SANGRER | |||
| BC-1 | Growth Inhibition Assay | IC50=42.6731 μM | SANGRER | |||
| GI-1 | Growth Inhibition Assay | IC50=42.9192 μM | SANGRER | |||
| NCI-H1694 | Growth Inhibition Assay | IC50=44.9472 μM | SANGRER | |||
| DG-75 | Growth Inhibition Assay | IC50=45.1577 μM | SANGRER | |||
| COR-L88 | Growth Inhibition Assay | IC50=45.2778 μM | SANGRER | |||
| LS-513 | Growth Inhibition Assay | IC50=45.9156 μM | SANGRER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=46.4612 μM | SANGRER | |||
| L-363 | Growth Inhibition Assay | IC50=46.881 μM | SANGRER | |||
| TE-6 | Growth Inhibition Assay | IC50=48.446 μM | SANGRER | |||
| NCI-H345 | Growth Inhibition Assay | IC50=48.468 μM | SANGRER | |||
| TE-5 | Growth Inhibition Assay | IC50=49.7118 μM | SANGRER | |||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells, IC50=0.048μM | 18630890 | |||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50=0.053μM | 18630890 | |||
| HT29 | Antiproliferative assay | Antiproliferative activity against human HT29 cells, IC50=0.15μM | 18630890 | |||
| HCT | Function assay | Inhibition of Aurora A in human HCT cells assessed as loss of autophosphorylation of Aurora A, IC50=0.31μM | 18630890 | |||
| HCT | Function assay | Inhibition of Aurora A assessed as separation of centrosomes in human HCT cells, IC50=0.31μM | 18630890 | |||
| HCT | Function assay | Inhibition of Aurora B assessed as loss of phospho histone H3 in human HCT cells, IC50=0.31μM | 18630890 | |||
| H29 | Function assay | Inhibition of Aurora B assessed as loss of phospho histone H3 in human H29 cells, IC50=0.74μM | 18630890 | |||
| HCT116 | Cytotoxicity assay | 10 to 14 days | Cytotoxicity against human HCT116 cells assessed as number of colonies after 10 to 14 days by colony forming assay, IC50=0.024μM | 19143567 | ||
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT116 cells assessed as distinct polyploidy phenotype after 72 hrs, Activity=0.03μM | 19143567 | ||
| COLO205 | Antiproliferative assay | Antiproliferative activity against human COLO205 cells by [3H]thymidine uptake assay, IC50=0.019μM | 19447622 | |||
| HCT116 | Cytotoxicity assay | Cytotoxicity against human HCT116 cells by MTS assay, IC50=0.12μM | 20550212 | |||
| HeLa | Function assay | Inhibition of phosphotransferase activity of recombinant aurora A expressed in HeLa cells, Ki=0.002μM | 20573509 | |||
| BA/F3 | Antiproliferative assay | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant, IC50=0.03μM | 20604564 | |||
| BA/F3 | Function assay | Inhibition of Bcr-Abl T315I mutant autophosphorylation in mouse BA/F3 cells, IC50=5μM | 20604564 | |||
| insect | Function assay | Inhibition of human recombinant His-tagged Aurora A kinase expressed in insect cells, IC50=0.0007μM | 21194953 | |||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50=0.028μM | 21802948 | |||
| HCT116 | Function assay | Inhibition of Aurora B kinase assessed as reduction in histone H3 phosphorylation in human HCT116 cells, IC50=0.055μM | 21802948 | |||
| HCT116 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay, IC50=0.3μM | 22572580 | ||
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=0.38μM | 22572580 | ||
| sf9 | Function assay | 15 mins | Inhibition of GST-tagged Aurora kinase A catalytic domain (123 to 401 amino acids) (unknown origin) expressed in sf9 cells using tetra(LRRWSLG) as substrate preincubated for 15 mins prior to substrate addition measured after 90 mins by luminescence assay, IC50=0.02μM | 23808327 | ||
| HCT116 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HCT116 cells after 96 hrs by MTS assay, EC50=0.12μM | 23808327 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50=0.12μM | 23808327 | |||
| HCT116 | Antitumor assay | 50 mg/kg | 5 days | Antitumor activity against human HCT116 cells xenografted in athymic nu/nu mouse assessed as reduction in tumor size at 50 mg/kg, iv qd for 5 days per week for 2 weeks measured twice a week | 23808327 | |
| HeLa | Function assay | 10 to 1000 nM | 48 hrs | Inhibition of Aurora kinase B in human HeLa cells assessed as delay in mitotic arrest by accumulation of multinucleated cells with 4N/8N DNA content at 10 to 1000 nM after 48 hrs by propidium iodide staining-based FACS flow cytometric analysis | 23808327 | |
| MOLT4 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MOLT4 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.0212μM | 24681066 | ||
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.036μM | 24681066 | ||
| HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HL60 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.0382μM | 24681066 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.0791μM | 24681066 | ||
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.127μM | 24681066 | ||
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.24μM | 24681066 | ||
| DU145 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human DU145 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.4μM | 24681066 | ||
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=1.3μM | 24681066 | ||
| HeLa | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HeLa cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=2.93μM | 24681066 | ||
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=3.05μM | 24681066 | ||
| PANC1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PANC1 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=4.13μM | 24681066 | ||
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=4.32μM | 24681066 | ||
| PC3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=5.81μM | 24681066 | ||
| SKBR3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SKBR3 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=9.99μM | 24681066 | ||
| NCI-N87 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-N87 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=11.6μM | 24681066 | ||
| HepG2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, TC50=3.3μM | 24910766 | ||
| HeLa | Function assay | 12 hrs | Inhibition of Aurora A in human HeLa cells after 12 hrs by ELISA method, IC50=0.261μM | 25812967 | ||
| HeLa | Function assay | 12 hrs | Inhibition of Aurora B in human HeLa cells after 12 hrs by ELISA method, IC50=0.453μM | 25812967 | ||
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50=19.4μM | 25812967 | ||
| HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50=27.3μM | 25812967 | ||
| HCT8 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT8 cells after 48 hrs by MTT assay, IC50=44.6μM | 25812967 | ||
| Hela | Function assay | Inhibition of recombinant Aurora A kinase derived from human Hela cells using kemptide as substrate in presence of [c-32P]ATP, Ki=0.002μM | 27884697 | |||
| NCI-H23 | Antiproliferative assay | Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant at | 28038940 | |||
| NCI-H358 | Antiproliferative assay | Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant at | 28038940 | |||
| U937 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human U937 cells after 48 hrs by CCK8 assay, IC50=0.036μM | 29358147 | ||
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay, IC50=0.079μM | 29358147 | ||
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by CCK8 assay, IC50=0.127μM | 29358147 | ||
| A431 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A431 cells after 48 hrs by CCK8 assay, IC50=0.24μM | 29358147 | ||
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by CCK8 assay, IC50=1.3μM | 29358147 | ||
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay, IC50=2.93μM | 29358147 | ||
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs by CCK8 assay, IC50=4.32μM | 29358147 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | |||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | |||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | |||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | |||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | |||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | |||
| L929sA | Function assay | 24 hrs | Inhibition of Aurk mouse L929sA cells transfected with human Fas assessed as reduction in cell growth after 24 hrs in presence of TNF by Hoechst 33342 staining-based microscopic assay, IC50=0.97μM | 29437386 | ||
| L929sA | Function assay | 0.5 hrs | Inhibition of RIPK1 in mouse L929sA cells transfected with human Fas assessed as inhibition in TNF-induced necroptosis pretreated for 0.5 hrs followed by TNF and zVAD.fmk addition measured after 3 hrs by Hoechst 33342/propidium iodide staining-based assay, IC50=0.98μM | 29437386 | ||
| L929sA | Function assay | 24 hrs | Inhibition of RIPK1 in mouse L929sA cells transfected with human Fas assessed as inhibition in TNF-induced necroptosis pretreated for 24 hrs followed by TNF and zVAD.fmk addition measured after 3 hrs by Hoechst 33342/propidium iodide staining-based assay, IC50=1.02μM | 29437386 | ||
| L929sA | Function assay | 24 hrs | Inhibition of Aurk mouse L929sA cells transfected with human Fas assessed as increase in nuclear area after 24 hrs in presence of TNF by Hoechst 33342 staining-based microscopic assay, IC50=1.06μM | 29437386 | ||
| HCT116 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=0.45μM | 30143423 | ||
| HCT15 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT15 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=1.23μM | 30143423 | ||
| HCT116 | Function assay | 100 nM | 24 hrs | Inhibition of cytokinesis in human HCT116 cells at 100 nM after 24 hrs by propidium iodide/RNase staining-based flow cytometric analysis | 30143423 | |
| HCT116 | Function assay | 1 uM | 24 hrs | Inhibition of cytokinesis in human HCT116 cells at 1 uM after 24 hrs by propidium iodide/RNase staining-based flow cytometric analysis | 30143423 | |
| HCT116 | Function assay | 1 uM | 3 hrs | Inhibition of Aurora B in human HCT116 cells assessed as reduction in histone H3 phosphorylation at Ser10 residue up to 1 uM after 3 hrs by Western blot analysis | 30143423 | |
| HCT116 | Function assay | 3 hrs | Inhibition of Aurora A phosphorylation at Thr288 residue in human HCT116 cells up to 1 uM after 3 hrs by Western blot analysis | 30143423 | ||
| HCT116 | Function assay | 3 hrs | Inhibition of Aurora B phosphorylation at Thr232 residue in human HCT116 cells up to 1 uM after 3 hrs by Western blot method | 30143423 | ||
| Sf9 | Function assay | Inhibition of GST-tagged AURORA A (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate, IC50=0.023μM | 30234987 | |||
| HeLa | Function assay | 12 hrs | Inhibition of Aurora A phosphorylation at Thr288 residue in human HeLa cells after 12 hrs by ELISA, IC50=0.013μM | 30502115 | ||
| HeLa | Function assay | 12 hrs | Inhibition of Aurora B phosphorylation at Thr232 residue in human HeLa cells after 12 hrs by ELISA, IC50=0.148μM | 30502115 | ||
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, GI50=35.8μM | 30502115 | ||
| LoVo | Antiproliferative assay | 48 hrs | Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay, GI50=45.3μM | 30502115 | ||
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, GI50=46.2μM | 30502115 | ||
| HeLa | Cell cycle assay | 5 uM | 12 hrs | Cell cycle arrest in human HeLa cells assessed as decrease in cyclin B1 protein expression at 5 uM after 12 hrs by Western blot analysis | 30502115 | |
| HeLa | Cell cycle assay | 5 uM | 12 hrs | Cell cycle arrest in human HeLa cells assessed as decrease in cdc2 protein expression at 5 uM after 12 hrs by Western blot analysis | 30502115 | |
| HeLa | Function assay | 5 uM | 12 hrs | Inhibition of Aurora A phosphorylation at Thr288 residue in human HeLa cells at 5 uM after 12 hrs by Western blot analysis | 30502115 | |
| HeLa | Function assay | 5 uM | 12 hrs | Inhibition of Aurora B phosphorylation at Thr232 residue in human HeLa cells at 5 uM after 12 hrs by Western blot analysis | 30502115 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50=35.8μM | 30728112 | ||
| LoVo | Antiproliferative assay | 48 hrs | Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay, IC50=45.3μM | 30728112 | ||
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, IC50=46.2μM | 30728112 | ||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
화학 정보, 보관 및 안정성
| 분자량 | 464.59 | 화학식 | C23H28N8OS |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 639089-54-6 | SDF 다운로드 | 원액 보관 |
|
|
| 동의어 | MK-0457 | Smiles | CC1=CC(=NN1)NC2=CC(=NC(=N2)SC3=CC=C(C=C3)NC(=O)C4CC4)N5CCN(CC5)C | ||
용해도
|
In vitro |
DMSO
: 93 mg/mL
(200.17 mM)
Ethanol : 40 mg/mL Water : Insoluble |
몰농도 계산기
희석 계산기
분자량 계산기
|
In vivo |
|||||
생체 내 제형 계산기 (투명한 용액)
1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
mg/kg
g
μL
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
계산 결과:
작업 농도: mg/ml;
DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.
참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.
작용 메커니즘
| Targets/IC50/Ki |
Aurora A
(Cell-free assay) 0.6 nM(Ki app)
Aurora C
(Cell-free assay) 4.6 nM(Ki app)
Aurora B
(Cell-free assay) 18 nM(Ki app)
FLT3
(Cell-free assay) 30 nM(Ki)
Bcr-Abl
(Cell-free assay) 30 nM(Ki)
|
|---|---|
| 시험관 내(In vitro) |
Tozasertib (VX-680)은 다중 키나제 프로파일에도 불구하고 약 300 nM의 IC50으로 유사한 세포독성을 유도하고 ABL 또는 FLT-3 (변이 및 야생형) 키나제로 형질감염된 BaF3 세포에서 G2/M 정지, 내재복제 및 apoptosis와 같은 AUR B 유사 억제 표현형을 나타냅니다. 이 화합물은 시간 의존적으로 CAL-62 증식을 억제합니다. 14일 동안의 치료는 8305C에서 약 70%, CAL-62, 8505C 및 BHT-101에서 90% 정도 콜로니 수와 크기를 유의하게 감소시킵니다. 다양한 ATC 세포를 이 화합물로 처리하면 25~150 nM 사이의 IC50으로 증식을 억제합니다. 이는 다양한 세포주가 연한 아가에서 콜로니를 형성하는 능력을 유의하게 손상시킵니다. caspase-3 활성 분석은 VX-680이 다양한 세포주에서 apoptosis를 유도한다는 것을 나타냅니다. 12시간 동안 화합물에 노출된 CAL-62 세포는 ≥4N DNA 함량을 가진 세포의 축적을 보였습니다. 타임랩스 분석은 처리된 CAL-62 세포가 분열하지 않고 중기에서 벗어나는 것을 보여줍니다. 또한, 이 치료 후 히스톤 H3 인산화는 폐지됩니다. 환자 유래 샘플에서 T315I 변이를 가진 BCR-Abl에 대해 유의미한 억제 활성을 가집니다.
|
| 키나아제 분석 |
키나제 억제 분석
|
|
ATP 소비는 피루브산 키나제/젖산 탈수소효소 효소 쌍을 통해 NADH 산화와 결합되며, 이는 340 nm에서의 흡광도 감소를 통해 모니터링할 수 있습니다. 반응물은 100 mM Tris (pH 8), 10 mM MgCl2, 2.2 mM ATP, 1 mM 포스포에놀피루브산, 0.6 mg/mL NADH, 75 units/mL 피루브산 키나제, 105 units/mL 젖산 탈수소효소, 그리고 0.5 mM 기질 펩타이드 (서열: EAIYAAPFAKKK)를 포함합니다. 반응 (75 μL)은 충분한 키나제를 첨가하여 반응물 농도를 30 nM 키나제 농도로 만들고, 흡광도 감소는 30°C에서 30분 동안 미세역가 플레이트 분광광도계에서 모니터링됩니다. 억제 상수는 100% DMSO 또는 DMSO 단독으로 Tozasertib (VX-680) 3.75 μL를 첨가하여 얻어집니다. Ki 값은 K i = IC50 / (1 + [S]/Kd)와 같이 계산되며, 여기서 [S] = [ATP] = 2.2 mM이고 Kd (ATP의 Abl에 대한) = 70 μM입니다. 이 값들은 야생형 및 H396P Abl 키나제 도메인에 대한 Kd (ATP)가 70 μM이라고 가정하여 계산됩니다.
|
|
| 생체 내(In vivo) |
Tozasertib (VX-680)은 인간 AML (HL-60) 이종이식 모델에서 종양 크기의 현저한 감소를 유발합니다. 누드 마우스에 75 mg/kg로 13일 동안 하루 두 번 복강내 주사(b.i.d. i.p.)로 처리했을 때, 평균 종양 부피가 98% 감소했습니다. 종양 성장 감소는 용량 의존적이며 12.5 mg/kg b.i.d. 용량에서 유의미합니다. 이 화합물은 잘 내약되며, 가장 높은 용량에서만 체중이 약간 감소하는 것이 관찰되었습니다. 또한 췌장 및 결장 이종이식 모델에서 종양 퇴행을 유발합니다. Tozasertib은 확립된 HCT116 종양을 가진 누드 쥐에 정맥 주사(i.v.)했을 때도 강력한 항종양 활성을 보입니다. 더 높은 용량(2 mg/kg/h)은 평균 종양 부피가 56% 감소하여 효능을 향상시킵니다.
|
참조 |
|
적용 분야
| 방법 | 바이오마커 | 이미지 | PMID |
|---|---|---|---|
| Western blot | DLK / p-MKK7 / MKK7 / p-JNK / JNK p-AURKA / AURKA / Survivin YAP p-AKT / p-GSK3β / Cleaved caspase-3 / Cleaved PARP |
|
23431148 |
| Immunofluorescence | α-tubulin / Aurora-A |
|
21600017 |
| Growth inhibition assay | Cell viability |
|
21600017 |
임상시험 정보
(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| NCT00290550 | Terminated | Carcinoma Non-Small-Cell Lung |
Merck Sharp & Dohme LLC |
June 2006 | Phase 2 |
| NCT00111683 | Completed | Chronic Myelogenous Leukemia in Blast Crisis|Lymphocytic Leukemia B Cell Acute|Myelodysplastic Syndromes|Myelogenous Leukemia Chronic |
Merck Sharp & Dohme LLC |
June 2005 | Phase 1 |
기술 지원
제품은 연구용으로만 사용됩니다. 인체에는 사용하지 마십시오. 환자에게 판매하지 않습니다.
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