연구용
제품 번호: S1153
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| LB771-HNC | Growth Inhibition Assay | IC50=48.9212 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=48.6202 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=48.4937 μM | SANGER | |||
| LB2518-MEL | Growth Inhibition Assay | IC50=47.0448 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=46.0115 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=44.9697 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=42.893 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=42.6671 μM | SANGER | |||
| DG-75 | Growth Inhibition Assay | IC50=42.6546 μM | SANGER | |||
| MLMA | Growth Inhibition Assay | IC50=42.2787 μM | SANGER | |||
| HT | Growth Inhibition Assay | IC50=42.0028 μM | SANGER | |||
| LC-1F | Growth Inhibition Assay | IC50=41.5705 μM | SANGER | |||
| NCI-H1882 | Growth Inhibition Assay | IC50=40.5998 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=39.5842 μM | SANGER | |||
| NCI-H345 | Growth Inhibition Assay | IC50=38.9106 μM | SANGER | |||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=38.2477 μM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=37.7069 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=37.6712 μM | SANGER | |||
| OPM-2 | Growth Inhibition Assay | IC50=37.2949 μM | SANGER | |||
| LU-139 | Growth Inhibition Assay | IC50=37.1856 μM | SANGER | |||
| COLO-684 | Growth Inhibition Assay | IC50=37.012 μM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=36.3276 μM | SANGER | |||
| TE-6 | Growth Inhibition Assay | IC50=36.3246 μM | SANGER | |||
| TE-441-T | Growth Inhibition Assay | IC50=36.1148 μM | SANGER | |||
| IMR-5 | Growth Inhibition Assay | IC50=35.3139 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=35.0861 μM | SANGER | |||
| TE-10 | Growth Inhibition Assay | IC50=34.9422 μM | SANGER | |||
| NCI-H2141 | Growth Inhibition Assay | IC50=34.6533 μM | SANGER | |||
| KGN | Growth Inhibition Assay | IC50=34.2524 μM | SANGER | |||
| LP-1 | Growth Inhibition Assay | IC50=33.8908 μM | SANGER | |||
| NCI-H64 | Growth Inhibition Assay | IC50=33.8597 μM | SANGER | |||
| RKO | Growth Inhibition Assay | IC50=33.5969 μM | SANGER | |||
| NCI-H526 | Growth Inhibition Assay | IC50=33.4936 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=32.9129 μM | SANGER | |||
| Calu-6 | Growth Inhibition Assay | IC50=32.4745 μM | SANGER | |||
| LOUCY | Growth Inhibition Assay | IC50=32.1253 μM | SANGER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=31.7535 μM | SANGER | |||
| SIG-M5 | Growth Inhibition Assay | IC50=31.6833 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=31.1397 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=31.1059 μM | SANGER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=31.0135 μM | SANGER | |||
| NCI-H510A | Growth Inhibition Assay | IC50=30.0329 μM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=29.9582 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=29.9483 μM | SANGER | |||
| KM12 | Growth Inhibition Assay | IC50=29.6239 μM | SANGER | |||
| GI-1 | Growth Inhibition Assay | IC50=29.0113 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=28.9733 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=28.908 μM | SANGER | |||
| TE-9 | Growth Inhibition Assay | IC50=28.7969 μM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=27.9869 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=27.9144 μM | SANGER | |||
| KARPAS-299 | Growth Inhibition Assay | IC50=26.8646 μM | SANGER | |||
| KURAMOCHI | Growth Inhibition Assay | IC50=26.8082 μM | SANGER | |||
| BL-41 | Growth Inhibition Assay | IC50=25.9597 μM | SANGER | |||
| NCI-H2126 | Growth Inhibition Assay | IC50=25.6529 μM | SANGER | |||
| HOP-62 | Growth Inhibition Assay | IC50=25.4425 μM | SANGER | |||
| IST-SL2 | Growth Inhibition Assay | IC50=24.5343 μM | SANGER | |||
| HH | Growth Inhibition Assay | IC50=24.3819 μM | SANGER | |||
| LS-513 | Growth Inhibition Assay | IC50=23.5179 μM | SANGER | |||
| EB-3 | Growth Inhibition Assay | IC50=23.1831 μM | SANGER | |||
| ACN | Growth Inhibition Assay | IC50=21.3389 μM | SANGER | |||
| NOMO-1 | Growth Inhibition Assay | IC50=21.2008 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=21.06 μM | SANGER | |||
| CESS | Growth Inhibition Assay | IC50=20.8549 μM | SANGER | |||
| BL-70 | Growth Inhibition Assay | IC50=20.3274 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=20.0356 μM | SANGER | |||
| BC-1 | Growth Inhibition Assay | IC50=19.1198 μM | SANGER | |||
| LC4-1 | Growth Inhibition Assay | IC50=18.8734 μM | SANGER | |||
| COLO-320-HSR | Growth Inhibition Assay | IC50=18.7688 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=18.3208 μM | SANGER | |||
| BC-3 | Growth Inhibition Assay | IC50=18.0305 μM | SANGER | |||
| TGW | Growth Inhibition Assay | IC50=17.8124 μM | SANGER | |||
| JAR | Growth Inhibition Assay | IC50=17.0152 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=16.8246 μM | SANGER | |||
| NCI-H1304 | Growth Inhibition Assay | IC50=16.3601 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=15.8382 μM | SANGER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=15.6482 μM | SANGER | |||
| HCC1599 | Growth Inhibition Assay | IC50=14.5975 μM | SANGER | |||
| SCC-3 | Growth Inhibition Assay | IC50=14.2956 μM | SANGER | |||
| RPMI-6666 | Growth Inhibition Assay | IC50=13.9121 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=13.8379 μM | SANGER | |||
| Raji | Growth Inhibition Assay | IC50=13.7894 μM | SANGER | |||
| RPMI-8402 | Growth Inhibition Assay | IC50=13.6262 μM | SANGER | |||
| GCIY | Growth Inhibition Assay | IC50=12.8613 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=12.6007 μM | SANGER | |||
| D-247MG | Growth Inhibition Assay | IC50=12.3516 μM | SANGER | |||
| NB1 | Growth Inhibition Assay | IC50=12.3308 μM | SANGER | |||
| COR-L279 | Growth Inhibition Assay | IC50=12.2907 μM | SANGER | |||
| LB831-BLC | Growth Inhibition Assay | IC50=11.5624 μM | SANGER | |||
| ST486 | Growth Inhibition Assay | IC50=10.351 μM | SANGER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=10.35 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=9.97495 μM | SANGER | |||
| KARPAS-422 | Growth Inhibition Assay | IC50=9.96336 μM | SANGER | |||
| Becker | Growth Inhibition Assay | IC50=9.46082 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=9.45785 μM | SANGER | |||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=8.50264 μM | SANGER | |||
| NCCIT | Growth Inhibition Assay | IC50=7.55482 μM | SANGER | |||
| MRK-nu-1 | Growth Inhibition Assay | IC50=7.12969 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=5.76116 μM | SANGER | |||
| 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 | 15958589 | |||
| LP-1 | Apoptosis assay | 30 uM | 3 hrs | Induction of apoptosis in human LP-1 cells at 30 uM after 3 hrs using TUNEL staining by flow cytometry | 15958589 | |
| LP-1 | Cytotoxicity assay | 20 to 30 uM | 24 hrs | Cytotoxicity against human LP-1 cells assessed as reduction of cell viability at 20 to 30 uM treated for 24 hrs followed by washout measured after total 72 hrs growth period alamar blue assay relative to control | 15958589 | |
| LP-1 | Apoptosis assay | 30 uM | 1.5 hrs | Induction of apoptosis in human LP-1 cells assessed as reduction of RNA polymerase 2 phosphoserine 2 level at 30 uM after 1.5 hrs by immunoblotting | 15958589 | |
| LP-1 | Apoptosis assay | 30 uM | 3 hrs | Induction of apoptosis in human LP-1 cells assessed as reduction of Mcl-1 protein level at 30 uM after 3 hrs by immunoblotting | 15958589 | |
| LP-1 | Apoptosis assay | 30 uM | 3 to 5 hrs | Induction of apoptosis in human LP-1 cells assessed as increase in level of cleaved PARP at 30 uM after 3 to 5 hrs by immunoblotting | 15958589 | |
| NCI-H929 | Apoptosis assay | 30 uM | 5 hrs | Induction of apoptosis in human NCI-H929 cells assessed as increase in level of cleaved PARP at 30 uM after 5 hrs by immunoblotting | 15958589 | |
| NCI-H929 | Apoptosis assay | 30 uM | 1.5 hrs | Induction of apoptosis in human NCI-H929 cells assessed as fast slow migrating hyperphosphorylated RNA polymerase 2O form at 30 uM after 1.5 hrs by immunoblotting | 15958589 | |
| RPM18226 | Apoptosis assay | 30 uM | 1.5 hrs | Induction of apoptosis in human RPM18226 cells assessed as reduction of RNA polymerase 2 phosphoserine 2 level at 30 uM after 1.5 hrs by immunoblotting | 15958589 | |
| RPM18226 | Apoptosis assay | 30 uM | 3 hrs | Induction of apoptosis in human RPM18226 cells assessed as reduction of Mcl-1 protein level at 30 uM after 3 hrs by immunoblotting | 15958589 | |
| RPM18226 | Apoptosis assay | 30 uM | 3 to 5 hrs | Induction of apoptosis in human RPM18226 cells assessed as increase in level of cleaved PARP at 30 uM after 3 to 5 hrs by immunoblotting | 15958589 | |
| NCI-H929 | Apoptosis assay | 30 uM | 3 hrs | Induction of apoptosis in human NCI-H929 cells assessed as changes in XIAP protein level at 30 uM after 3 hrs by immunoblotting | 15958589 | |
| NCI-H929 | Apoptosis assay | 30 uM | 3 hrs | Induction of apoptosis in human NCI-H929 cells assessed as changes in survivin protein level at 30 uM after 3 hrs by immunoblotting | 15958589 | |
| RPM18226 | Apoptosis assay | 30 uM | 3 hrs | Induction of apoptosis in human RPM18226 cells at 30 uM after 3 hrs using TUNEL staining by flow cytometry | 15958589 | |
| NCI-H929 | Apoptosis assay | 30 uM | 1.5 hrs | Induction of apoptosis in human NCI-H929 cells assessed as reduction of RNA polymerase 2 phosphoserine 2 level at 30 uM after 1.5 hrs by immunoblotting | 15958589 | |
| NCI-H929 | Apoptosis assay | 30 uM | 1.5 hrs | Induction of apoptosis in human NCI-H929 cells assessed as dephosphorylation of pRb at S249/T252 at 30 uM after 1.5 hrs by immunoblotting | 15958589 | |
| NCI-H929 | Cytotoxicity assay | 20 to 30 uM | 16 hrs | Cytotoxicity against human NCI-H929 cells assessed as reduction of cell viability at 20 to 30 uM treated for 16 hrs followed by washout measured after total 72 hrs growth period alamar blue assay relative to control | 15958589 | |
| NCI-H929 | Apoptosis assay | 30 uM | 3 hrs | Induction of apoptosis in human NCI-H929 cells assessed as reduction of Mcl-1 protein level at 30 uM after 3 hrs by immunoblotting | 15958589 | |
| NCI-H929 | Apoptosis assay | 30 uM | 3 hrs | Induction of apoptosis in human NCI-H929 cells assessed as changes in Bcl-2 protein level at 30 uM after 3 hrs by immunoblotting | 15958589 | |
| NCI-H929 | Apoptosis assay | 30 uM | 3 hrs | Induction of apoptosis in human NCI-H929 cells at 30 uM after 3 hrs using TUNEL staining by flow cytometry | 15958589 | |
| NCI-H929 | Apoptosis assay | 30 uM | 1.5 hrs | Induction of apoptosis in human NCI-H929 cells assessed as reduction of RNA polymerase 2 phosphoserine 5 level at 30 uM after 1.5 hrs by immunoblotting | 15958589 | |
| NCI-H929 | Apoptosis assay | 30 uM | 1.5 hrs | Induction of apoptosis in human NCI-H929 cells assessed as reduction of Hdm2 level at 30 uM after 1.5 hrs by immunoblotting | 15958589 | |
| NCI-H929 | Apoptosis assay | 30 uM | 1.5 hrs | Induction of apoptosis in human NCI-H929 cells assessed as increase of p53 accumulation at 30 uM after 1.5 hrs by immunoblotting | 15958589 | |
| 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 | 21080703 | |||
| HCT116 | Function assay | 30 to 40 umol/L | 24 hrs | Inhibition of cyclin A in human HCT116 cells assessed as decrease in protein level at 30 to 40 umol/L after 24 hrs by immunoblotting analysis | 21080703 | |
| HCT116 | Function assay | 30 to 40 umol/L | 24 hrs | Inhibition of cyclin B in human HCT116 cells assessed as decrease in protein level at 30 to 40 umol/L after 24 hrs by immunoblotting analysis | 21080703 | |
| HCT116 | Function assay | 30 to 40 umol/L | 24 hrs | Inhibition of cyclin D1 in human HCT116 cells assessed as decrease in protein level at 30 to 40 umol/L after 24 hrs by immunoblotting analysis | 21080703 | |
| HCT116 | Function assay | 30 to 40 umol/L | 24 hrs | Inhibition of CDK2 in human HCT116 cells assessed as decrease in protein level at 30 to 40 umol/L after 24 hrs by immunoblotting analysis | 21080703 | |
| HT-29 | Function assay | 2.5 to 40 uM | 24 hrs | Inhibition of retinoblastoma protein in human HT-29 cells assessed as reduction of cyclin A level at 2.5 to 40 uM after 24 hrs by immunoblotting | 21417417 | |
| MCF7 | Cell cycle assay | 24 hrs | Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide and BrdU staining by flow cytometry | 21417417 | ||
| RPMI8226 | Cell cycle assay | 24 hrs | Cell cycle arrest in human RPMI8226 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide and BrdU staining by flow cytometry | 21417417 | ||
| MCF7 | Cell cycle assay | 24 hrs | Cell cycle arrest in human MCF7 cells assessed as decrease in S phase cell population after 24 hrs using propidium iodide and BrdU staining by flow cytometry | 21417417 | ||
| MCF7 | Cell cycle assay | 24 hrs | Cell cycle arrest in human MCF7 cells assessed as accumulation at sub-G1 phase after 24 hrs using propidium iodide and BrdU staining by flow cytometry | 21417417 | ||
| RPMI8226 | Cell cycle assay | 24 hrs | Cell cycle arrest in human RPMI8226 cells assessed as accumulation at sub-G1 phase after 24 hrs using propidium iodide and BrdU staining by flow cytometry | 21417417 | ||
| MCF7 | Cell cycle assay | 80 uM | 24 hrs | Cell cycle arrest in human MCF7 cells assessed as reduction of actively replicating DNA level at 80 uM after 24 hrs using propidium iodide and BrdU staining by flow cytometry | 21417417 | |
| MCF7 | Function assay | 20 uM | 24 hrs | Induction of p53-dependent transcriptional activity in human MCF7 cells assessed as increase of p21 WAF1 level at 20 uM after 24 hrs by immunofluorescence assay | 21417417 | |
| RPMI8226 | Cell cycle assay | 24 hrs | Cell cycle arrest in human RPMI8226 cells assessed as decrease in S phase cell population after 24 hrs using propidium iodide and BrdU staining by flow cytometry | 21417417 | ||
| RPMI8226 | Cell cycle assay | 80 uM | 24 hrs | Cell cycle arrest in human RPMI8226 cells assessed as reduction of actively replicating DNA level at 80 uM after 24 hrs using propidium iodide and BrdU staining by flow cytometry | 21417417 | |
| A549 | Apoptosis assay | 2 uM | 48 hrs | Induction of apoptosis in human A549 cells assessed as DNA fragmentation at 2 uM after 48 hrs by agarose gel electrophoresis | 23623491 | |
| Sf9 | Function assay | 10 mins | Inhibition of His-6-tagged recombinant human CDK2/cyclinE expressed in baculovirus-infected sf9 cells using histone H1 as substrate after 10 mins by liquid scintillation counting in presence of [gamma-32P]ATP, IC50 = 0.1 μM. | 24417566 | ||
| BJ | Function assay | 10 uM | 10 days | Suppression of senescence in human BJ cells assessed as increase in cell number at 10 uM after 10 days by senescence reversal assay | 24681986 | |
| BJ | Function assay | 10 uM | 10 days | Inhibition of ataxia telangiectasia-mutated in human BJ cells assessed as increase in cell number at 10 uM after 10 days by senescence reversal assay | 24681986 | |
| MCF7 | Function assay | 10 uM | 10 mins | Sensitization of infrared-induced DNA damage in human MCF7 cells assessed as reduction in colony formation at 10 uM pretreated for 10 mins followed by irradiation for 4 hrs measured after 10 days by crystal violet staining analysis | 26851505 | |
| Caco2 | Cell cycle assay | Cell cycle arrest in human Caco2 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay | 28214231 | |||
| HaCaT | Cell cycle assay | Cell cycle arrest in human HaCaT cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay | 28214231 | |||
| HuH7 | Cell cycle assay | Cell cycle arrest in human HuH7 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay | 28214231 | |||
| PC3 | Cell cycle assay | Cell cycle arrest in human PC3 cells assessed as accumulation at G2/M phase by Hoechst staining based fluorescence assay | 28214231 | |||
| MDA-MB-231 | Cell cycle assay | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay | 28214231 | |||
| HCT116 | Cell cycle assay | Cell cycle arrest in human HCT116 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay | 28214231 | |||
| 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 | 28557430 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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 | |||
| 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 | 30199702 | |||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
| 분자량 | 354.45 | 화학식 | C19H26N6O |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 186692-46-6 | SDF 다운로드 | 원액 보관 |
|
|
| 동의어 | CYC202, Seliciclib, R-roscovitine | Smiles | CCC(CO)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)NCC3=CC=CC=C3 | ||
|
In vitro |
DMSO
: 71 mg/mL
(200.31 mM)
Ethanol : 71 mg/mL Water : Insoluble |
|
In vivo |
|||||
1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
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.
| Targets/IC50/Ki |
CDK5/p35
(Cell-free assay) 0.16 μM
Cdc2/CyclinB
(Cell-free assay) 0.65 μM
CDK2/CyclinA
(Cell-free assay) 0.7 μM
CDK2/CyclinE
(Cell-free assay) 0.7 μM
ERK2
(Cell-free assay) 14 μM
|
|---|---|
| 시험관 내(In vitro) |
Roscovitine (Seliciclib)은 cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E 및 cdk5/p53에 대해 각각 0.65, 0.7, 0.7 및 0.16 μM의 IC50 값으로 일부 CDK에 대해 높은 효율성과 높은 선택성을 나타냅니다. 이 화합물은 불가사리 난모세포와 성게 배아의 마이크로몰 범위에서 전중기-중기 전환을 가역적으로 억제하고, Xenopus 난 추출물에서 in vitro M-phase-promoting factor 활성과 in vitro DNA 합성을 억제하며, 평균 16 μM의 IC50으로 포유류 세포주의 증식을 억제합니다. 메산지움 세포에서 이 화합물은 CDK2 활성의 용량 의존적 감소를 유발하며, 7.5, 12.5 및 25 mM 농도에서 각각 25%, 50%, 100%의 CDK2 활성 감소를 야기합니다. 최근 연구에 따르면 이 화합물은 Dictyostelium discoideum에서 무균 성장 중 cdk5 단백질 발현에는 영향을 미치지 않으면서 cdk5 kinase 활성, 세포 증식, 다세포 발달 및 cdk5 핵 이동을 억제하는 것으로 나타났습니다. |
| 키나아제 분석 |
효소
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| 생체 내(In vivo) |
Roscovitine (Seliciclib)은 50 mg/kg 용량에서 유잉 육종 계열 종양(ESFT) 이종 이식편의 성장을 유의미하게 억제합니다. 이 화합물은 확립된 MCF7 이종 이식편을 보유한 누드 마우스에서 세포 사멸(apoptosis)보다는 Cell Cycle 정지를 포함하는 메커니즘을 통해 독성 증가 없이 doxorubicin의 항종양 효과를 향상시킵니다. |
참조 |
|
| 방법 | 바이오마커 | 이미지 | PMID |
|---|---|---|---|
| Western blot | p-Rb / p-CDK2 / CDK2 / Cyclin D1 / Cyclin A2 / ERα / ERβ/ AIB1 / PELP1 pT231-tau / pS202-tau / tau |
|
21834972 |
| Immunofluorescence | E2F1 / FASN / Bmi1 / Cyclin D2 / CDK2 / CDK4 CDK1 / Smek2 / FUBP1 / Cdc20 |
|
20890301 |
| Growth inhibition assay | Cell viability |
|
29996940 |
(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| NCT02649751 | Terminated | Cystic Fibrosis |
University Hospital Brest|ManRos Therapeutics|Cyclacel Pharmaceuticals Inc. |
February 22 2016 | Phase 2 |
질문 1:
How can I reconstitute it for in vivo studies?
답변:
It in 1% DMSO+10% Tween 80+20% N-N-dimethylacetamide+PEG 400 is a clear solution which is okay for injection. And this compound in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30mg/ml is a suspension, which is fine for oral gavage.