연구용
제품 번호S1006
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| CTV-1 | Growth Inhibition Assay | IC50=0.06143 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=0.1599 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=0.23688 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=0.265 μM | SANGER | |||
| TE-15 | Growth Inhibition Assay | IC50=0.27412 μM | SANGER | |||
| NCI-H1648 | Growth Inhibition Assay | IC50=0.28116 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=0.3268 μM | SANGER | |||
| LB996-RCC | Growth Inhibition Assay | IC50=0.44196 μM | SANGER | |||
| K-562 | Growth Inhibition Assay | IC50=0.44967 μM | SANGER | |||
| D-336MG | Growth Inhibition Assay | IC50=0.50304 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=0.60529 μM | SANGER | |||
| EW-24 | Growth Inhibition Assay | IC50=0.62693 μM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=0.65249 μM | SANGER | |||
| NCCIT | Growth Inhibition Assay | IC50=0.73218 μM | SANGER | |||
| NCI-H1436 | Growth Inhibition Assay | IC50=0.79049 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=0.86203 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=0.87275 μM | SANGER | |||
| A704 | Growth Inhibition Assay | IC50=0.8921 μM | SANGER | |||
| TK10 | Growth Inhibition Assay | IC50=0.90669 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=1.19779 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=1.20507 μM | SANGER | |||
| RXF393 | Growth Inhibition Assay | IC50=1.2436 μM | SANGER | |||
| KGN | Growth Inhibition Assay | IC50=1.27687 μM | SANGER | |||
| NB69 | Growth Inhibition Assay | IC50=1.37497 μM | SANGER | |||
| TE-11 | Growth Inhibition Assay | IC50=1.43418 μM | SANGER | |||
| TE-1 | Growth Inhibition Assay | IC50=1.44105 μM | SANGER | |||
| ST486 | Growth Inhibition Assay | IC50=1.45852 μM | SANGER | |||
| HOP-62 | Growth Inhibition Assay | IC50=1.50246 μM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=1.55083 μM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=1.55453 μM | SANGER | |||
| TE-10 | Growth Inhibition Assay | IC50=1.66252 μM | SANGER | |||
| RL95-2 | Growth Inhibition Assay | IC50=1.66902 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=1.71782 μM | SANGER | |||
| MFH-ino | Growth Inhibition Assay | IC50=1.7787 μM | SANGER | |||
| GB-1 | Growth Inhibition Assay | IC50=1.79833 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=1.84688 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=1.88574 μM | SANGER | |||
| SW982 | Growth Inhibition Assay | IC50=1.92093 μM | SANGER | |||
| KALS-1 | Growth Inhibition Assay | IC50=1.98722 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=2.05958 μM | SANGER | |||
| GI-1 | Growth Inhibition Assay | IC50=2.16084 μM | SANGER | |||
| SW962 | Growth Inhibition Assay | IC50=2.17178 μM | SANGER | |||
| SW872 | Growth Inhibition Assay | IC50=2.18507 μM | SANGER | |||
| NCI-H747 | Growth Inhibition Assay | IC50=2.25714 μM | SANGER | |||
| MZ1-PC | Growth Inhibition Assay | IC50=2.29356 μM | SANGER | |||
| MSTO-211H | Growth Inhibition Assay | IC50=2.35723 μM | SANGER | |||
| BL-70 | Growth Inhibition Assay | IC50=2.47422 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=2.57408 μM | SANGER | |||
| SNB75 | Growth Inhibition Assay | IC50=2.68594 μM | SANGER | |||
| IST-SL2 | Growth Inhibition Assay | IC50=2.72379 μM | SANGER | |||
| GCIY | Growth Inhibition Assay | IC50=2.87005 μM | SANGER | |||
| KU812 | Growth Inhibition Assay | IC50=3.05299 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=3.12109 μM | SANGER | |||
| ETK-1 | Growth Inhibition Assay | IC50=3.20767 μM | SANGER | |||
| SF126 | Growth Inhibition Assay | IC50=3.31174 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=3.557 μM | SANGER | |||
| KNS-42 | Growth Inhibition Assay | IC50=3.65 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=3.73433 μM | SANGER | |||
| PF-382 | Growth Inhibition Assay | IC50=3.83698 μM | SANGER | |||
| SH-4 | Growth Inhibition Assay | IC50=4.25259 μM | SANGER | |||
| KM12 | Growth Inhibition Assay | IC50=4.32416 μM | SANGER | |||
| NB5 | Growth Inhibition Assay | IC50=4.41864 μM | SANGER | |||
| KURAMOCHI | Growth Inhibition Assay | IC50=4.65256 μM | SANGER | |||
| Becker | Growth Inhibition Assay | IC50=4.66416 μM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=4.81344 μM | SANGER | |||
| KINGS-1 | Growth Inhibition Assay | IC50=4.82373 μM | SANGER | |||
| LS-123 | Growth Inhibition Assay | IC50=5.49684 μM | SANGER | |||
| SF268 | Growth Inhibition Assay | IC50=5.61262 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=5.63667 μM | SANGER | |||
| NMC-G1 | Growth Inhibition Assay | IC50=6.01811 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=6.02075 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=6.53074 μM | SANGER | |||
| SR | Growth Inhibition Assay | IC50=6.58807 μM | SANGER | |||
| BB49-HNC | Growth Inhibition Assay | IC50=6.73206 μM | SANGER | |||
| KLE | Growth Inhibition Assay | IC50=6.78377 μM | SANGER | |||
| HUTU-80 | Growth Inhibition Assay | IC50=6.98466 μM | SANGER | |||
| SNU-C2B | Growth Inhibition Assay | IC50=7.82737 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=7.94904 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=8.42808 μM | SANGER | |||
| GDM-1 | Growth Inhibition Assay | IC50=8.97292 μM | SANGER | |||
| LC4-1 | Growth Inhibition Assay | IC50=9.00911 μM | SANGER | |||
| MLMA | Growth Inhibition Assay | IC50=9.15006 μM | SANGER | |||
| EoL-1-cell | Growth Inhibition Assay | IC50=9.30192 μM | SANGER | |||
| BOKU | Growth Inhibition Assay | IC50=9.96466 μM | SANGER | |||
| EVSA-T | Growth Inhibition Assay | IC50=10.6568 μM | SANGER | |||
| D-283MED | Growth Inhibition Assay | IC50=10.9176 μM | SANGER | |||
| NB1 | Growth Inhibition Assay | IC50=11.0242 μM | SANGER | |||
| RPMI-8402 | Growth Inhibition Assay | IC50=11.178 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=11.1806 μM | SANGER | |||
| NB7 | Growth Inhibition Assay | IC50=11.3297 μM | SANGER | |||
| RPMI-6666 | Growth Inhibition Assay | IC50=12.9567 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=13.2701 μM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=13.5948 μM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=13.9234 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=14.3915 μM | SANGER | |||
| SKM-1 | Growth Inhibition Assay | IC50=14.4499 μM | SANGER | |||
| TE-6 | Growth Inhibition Assay | IC50=14.7591 μM | SANGER | |||
| LB771-HNC | Growth Inhibition Assay | IC50=14.7898 μM | SANGER | |||
| ECC4 | Growth Inhibition Assay | IC50=17.0277 μM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=17.4655 μM | SANGER | |||
| LB647-SCLC | Growth Inhibition Assay | IC50=17.4949 μM | SANGER | |||
| NB10 | Growth Inhibition Assay | IC50=18.5256 μM | SANGER | |||
| L-540 | Growth Inhibition Assay | IC50=18.8109 μM | SANGER | |||
| NCI-H2126 | Growth Inhibition Assay | IC50=19.51 μM | SANGER | |||
| HH | Growth Inhibition Assay | IC50=20.0099 μM | SANGER | |||
| MPP-89 | Growth Inhibition Assay | IC50=23.2289 μM | SANGER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=23.8658 μM | SANGER | |||
| KP-N-YS | Growth Inhibition Assay | IC50=23.9255 μM | SANGER | |||
| EC-GI-10 | Growth Inhibition Assay | IC50=24.5989 μM | SANGER | |||
| EKVX | Growth Inhibition Assay | IC50=26.0203 μM | SANGER | |||
| TGBC1TKB | Growth Inhibition Assay | IC50=26.434 μM | SANGER | |||
| Daudi | Growth Inhibition Assay | IC50=27.0773 μM | SANGER | |||
| ALL-PO | Growth Inhibition Assay | IC50=27.081 μM | SANGER | |||
| NB6 | Growth Inhibition Assay | IC50=27.488 μM | SANGER | |||
| ES6 | Growth Inhibition Assay | IC50=27.9123 μM | SANGER | |||
| COLO-320-HSR | Growth Inhibition Assay | IC50=28.0373 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=28.1287 μM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=28.7773 μM | SANGER | |||
| LC-1F | Growth Inhibition Assay | IC50=29.7346 μM | SANGER | |||
| SCLC-21H | Growth Inhibition Assay | IC50=30.7317 μM | SANGER | |||
| SK-PN-DW | Growth Inhibition Assay | IC50=32.5598 μM | SANGER | |||
| D-247MG | Growth Inhibition Assay | IC50=32.9773 μM | SANGER | |||
| TE-5 | Growth Inhibition Assay | IC50=33.0362 μM | SANGER | |||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=33.5048 μM | SANGER | |||
| LB2518-MEL | Growth Inhibition Assay | IC50=33.7666 μM | SANGER | |||
| LOXIMVI | Growth Inhibition Assay | IC50=33.7928 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=35.144 μM | SANGER | |||
| A253 | Growth Inhibition Assay | IC50=35.7429 μM | SANGER | |||
| HCC1599 | Growth Inhibition Assay | IC50=36.7053 μM | SANGER | |||
| EB-3 | Growth Inhibition Assay | IC50=36.9518 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=37.3224 μM | SANGER | |||
| SW684 | Growth Inhibition Assay | IC50=41.8495 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=42.0522 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=42.1676 μM | SANGER | |||
| TE-9 | Growth Inhibition Assay | IC50=43.4596 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=44.3925 μM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=44.5034 μM | SANGER | |||
| RCC10RGB | Growth Inhibition Assay | IC50=44.7392 μM | SANGER | |||
| CP67-MEL | Growth Inhibition Assay | IC50=45.6241 μM | SANGER | |||
| NB17 | Growth Inhibition Assay | IC50=45.6643 μM | SANGER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=45.9464 μM | SANGER | |||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=46.0119 μM | SANGER | |||
| HCE-4 | Growth Inhibition Assay | IC50=46.5968 μM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=46.7682 μM | SANGER | |||
| KARPAS-422 | Growth Inhibition Assay | IC50=47.0895 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=47.1622 μM | SANGER | |||
| HCE-T | Growth Inhibition Assay | IC50=47.6828 μM | SANGER | |||
| PSN1 | Growth Inhibition Assay | IC50=47.7813 μM | SANGER | |||
| NIH3T3 | Function assay | Inhibition of human c-Src in NIH3T3 cells, IC50 = 0.0027 μM. | 17064066 | |||
| HEK293 | Function assay | 1 hr | Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki = 0.0398 μM. | 29941193 | ||
| HEK293 | Function assay | 1 hr | Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50 = 0.418 μM. | 29941193 | ||
| Rh30 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human Rh30 cells after 48 hrs by CellTiter-Glo luminescent assay, IC50 = 10.1 μM. | 23787099 | ||
| Huh7 | Antiviral assay | 2.5 uM | 5 days | Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control | 17360676 | |
| Huh7 | Antiviral assay | 2.5 uM | 6 days | Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control | 17360676 | |
| Vero | Antiviral assay | 2.5 uM | 4 days | Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control | 17360676 | |
| Vero | Antiviral assay | 2.5 uM | 6 days | Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control | 17360676 | |
| C6/36 | Antiviral assay | 2.5 uM | 4 days | Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control | 17360676 | |
| C6/36 | Antiviral assay | 2.5 uM | 5 days | Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control | 17360676 | |
| Vero | Antiviral assay | 3 days | Antiviral activity against Dengue virus infected in african green monkey Vero cells administered after viral challenge after 3 days by viral plaque assay | 17360676 | ||
| Vero | Antiviral assay | 2.5 uM | 5 days | Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control | 17360676 | |
| Huh7 | Antiviral assay | 2.5 uM | 4 days | Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control | 17360676 | |
| C6/36 | Antiviral assay | 2.5 uM | 6 days | Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control | 17360676 | |
| HEK293 | Function assay | 0.1 to 1 uM | 16 hrs | Inhibition of collagen I-induced DDR2 (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting | 26191369 | |
| 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 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 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 | |||
| 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 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| HEK293 | Function assay | 0.1 to 1 uM | 16 hrs | Inhibition of collagen I-induced DDR2 I638F mutant (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting | 26191369 | |
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
| 분자량 | 542.03 | 화학식 | C27H32ClN5O5 |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 379231-04-6 | SDF 다운로드 | 원액 보관 |
|
|
| 동의어 | N/A | Smiles | CN1CCN(CC1)CCOC2=CC3=C(C(=C2)OC4CCOCC4)C(=NC=N3)NC5=C(C=CC6=C5OCO6)Cl | ||
|
In vitro |
DMSO
: 100 mg/mL
(184.49 mM)
Ethanol : 100 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.
| 특징 |
The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.
|
|---|---|
| Targets/IC50/Ki |
c-Src
(Cell-free assay) 2.7 nM
LCK
(Cell-free assay) <4 nM
c-YES
(Cell-free assay) 4 nM
EGFR (L861Q)
(Cell-free assay) 4 nM
Lyn
(Cell-free assay) 5 nM
EGFR (L858R)
(Cell-free assay) 5 nM
Fyn
(Cell-free assay) 10 nM
FGR
(Cell-free assay) 10 nM
BLK
(Cell-free assay) 11 nM
v-Abl
(Cell-free assay) 30 nM
EGFR
(Cell-free assay) 66 nM
c-Kit
(Cell-free assay) 200 nM
EphA2
(Cell-free assay) 236 nM
|
| 시험관 내(In vitro) |
Saracatinib (AZD0530)은 또한 c-Yes, Fyn, Lyn, Blk, Fgr, Lck를 포함한 다른 Src 티로신 키나아제 계열 구성원을 IC50 4-10 nM로 강력하게 억제합니다. Src Y530F NIH 3T3를 IC50 80 nM으로 민감하게 억제합니다. 이 화합물은 3차원 콜라겐 매트릭스를 통한 HT1080 세포의 침윤을 유의하게 손상시키고 NBT-II 방광암 세포에서 EGF 유도 세포 확산을 완전히 억제합니다. Y419 인산화 억제를 통해 DU145 및 PC3 세포에서 Src 활성화를 강력하게 억제합니다. LAPC-4, PZ-HPV7 및 RWPE-1 세포에서는 낮은 활성을 보이는 반면 PC3, DU145, CWR22Rv1 및 LNCaP를 포함한 전립선암의 성장을 억제합니다. G1/S에서 세포 주기 정지를 유도하지만 caspase 3 절단은 유도하지 않습니다. 또한 Boyden 챔버에서 DU145 및 PC3 이동을 유의하게 억제합니다. AKT의 강력하고 지속적인 차단을 제공하고 A549 및 Calu-6 세포에서 방사선에 대한 민감도를 향상시킵니다. 활동, 재흡수 및 형성에서 파골세포를 억제합니다. 또한 파골세포 전구체 이동을 가역적으로 방지합니다. |
| 키나아제 분석 |
키나아제 분석
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티로신 키나아제 활성의 IC50은 수용체 및 비수용체 티로신 키나아제 패널의 재조합 촉매 도메인을 사용한 효소 연결 면역흡착 분석(ELISA)으로 측정됩니다(일부 경우에는 촉매 도메인의 일부만 사용됩니다). 이 화합물은 0.001-10 mM 범위로 투여됩니다. 세린/트레오닌 키나아제 패널에 대한 특이성 분석은 32P를 사용한 필터 포획 분석을 사용하여 수행됩니다. 간략하게, 0.5 μL Saracatinib (AZD0530) 또는 대조군(DMSO 단독 또는 pH 3.0 버퍼 대조군)을 포함하는 멀티드롭 384 플레이트를 15 μL의 효소와 펩타이드/단백질 기질과 함께 5분 동안 배양한 후 10 μL의 20 mM Mg-ATP를 첨가하여 반응을 시작합니다. 모든 효소에 대해 최종 농도는 Michaelis 상수(Km)에 근접하게 됩니다. 분석은 실온에서 30분 동안 수행된 후 5 μL의 인산을 첨가하여 종료됩니다. 혼합 후, 웰 내용은 인산을 세척 완충액으로 사용하여 P81 Unifilter 플레이트에 수확됩니다. 그런 다음 IC50이 계산됩니다.
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| 생체 내(In vivo) |
Saracatinib (AZD0530)은 Src3T3 동종이식편에서 뛰어난 종양 성장 억제를 보이며 Calu-6, MDA-MB-231, AsPc-1 및 BT474C 이종이식편에서 중간 정도의 성장 지연을 보입니다. 이 화합물은 또한 25mg/kg (경구 투여, 매일) 용량으로 정위 DU145 이종이식 마우스에서 뛰어난 항종양 활성을 보입니다. |
참조 |
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| 방법 | 바이오마커 | 이미지 | PMID |
|---|---|---|---|
| Western blot | pY576-FAK / pY861-FAK / FAK pY418 Src / Src / pY410 CAS / CAS / Py421 Cortactin / Cortactin p-Akt / p-mTOR / Akt / mTOR / p-S6 / S6 / p-AMPKα / AMPKα |
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20551056 |
| Growth inhibition assay | Cell number |
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24349321 |
(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| NCT04598919 | Active not recruiting | Idiopathic Pulmonary Fibrosis (IPF) |
National Jewish Health|Yale University|Icahn School of Medicine at Mount Sinai|AstraZeneca|National Center for Advancing Translational Sciences (NCATS)|Baylor University|International Center for Health Outcomes and Innovation Research |
November 12 2020 | Phase 1|Phase 2 |
| NCT04307953 | Recruiting | Fibrodysplasia Ossificans Progressiva |
Amsterdam UMC location VUmc|Royal National Orthopaedic Hospital NHS Trust|Klinikum Garmisch-Patenkirchen|University of Oxford|Brigham and Women''s Hospital|AstraZeneca|Innovative Medicines Initiative |
August 5 2020 | Phase 2 |
| NCT02085603 | Completed | Cancer |
Sheffield Teaching Hospitals NHS Foundation Trust|AstraZeneca |
March 2014 | Phase 2 |
| NCT01864655 | Completed | Alzheimer''s Disease |
Stephen M. Strittmatter|National Institute of Neurological Disorders and Stroke (NINDS)|Yale University |
July 2013 | Phase 1 |
| NCT01000896 | Withdrawn | Cancer|Non Small Cell Lung Cancer|Epithelial Ovarian Cancer |
AstraZeneca |
January 2010 | Phase 1 |
질문 1:
What is its half-life?
답변:
Based on the following paper, its half-life in vivo is around 40 hours and it reaches its peak level around 2–4 hours after dosing: http://clincancerres.aacrjournals.org/content/16/19/4876.long