GDC0575(ARRY-575,RG7441)
产品编号: DC10485
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应用领域
GDC-0575 (ARRY-575, RG7741) 是高选择性,有口服活性的小分子 Chk1 抑制剂,其在异种移植模型中导致肿瘤缩小和生长延迟,IC50 值为1.2 nM。
Cas No.: |
1196541-47-5 |
名称: |
N-[4-[(3R)-3-amino-1-piperidinyl]-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl]- |
别名: |
GDC0575,ARRY 575,RG7-441,GDC 0575,ARRY575,RG 7441,GDC-0575,ARRY-575,RG744 |
SMILES: |
O=C(C1CC1)NC2=CNC3=NC=C(Br)C(N4C[C@H](N)CCC4)=C32 |
分子式: |
C16H20BrN5O |
分子量: |
378.27 |
纯度: |
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保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: |
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References: |
GDC0575(ARRY-575,RG7441)is a small molecule inhibitor of cell cycle checkpoint kinase 1 (Chk1), with potential chemosensitization activity. Chk1 inhibitor GDC-0575 specifically binds to and inhibits Chk1; this may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases, which permits the cells to undergo DNA repair prior to entry into mitosis. Therefore, Chk1 inhibition may sensitize tumor cells to the DNA damaging effects of certain chemotherapeutic agents. Chk1 is an ATP-dependent serine-threonine kinase that phosphorylates cdc25 phosphatases in response to DNA damage. This results in both inhibitory tyrosine phosphorylation of cyclin-dependent kinase (CDK)-cyclin complexes and cell cycle arrest, which facilitates DNA damage repair. |
Kinase Assay: |
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References: |
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MSDS
COA
LOT NO. |
DOWNLOAD |
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2018-0101 |
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