GDC-0575

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Chemical Structure| 1196541-47-5 同义名 : ARRY-575;RG7741
CAS号 : 1196541-47-5
货号 : A690852
分子式 : C16H20BrN5O
纯度 : 99%+
分子量 : 378.267
MDL号 : MFCD29048675
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(277.58 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Chk1 (Checkpoint kinase 1), an important serine/threonine kinase, is responding to DNA damage and stall DNA replication. Chk1 plays a key role in maintaining the replication fork viability during exposure to DNA antimetabolites. Inhibition of Chk1 will lead to accumulation of double-strand DNA breaks and cell death in human tumor cell lines exposure to antimetabolite. GDC-0575 is a selective Chk1 inhibitor with IC50 value of 1.2 nM. GDC-0575 exhibited anti-proliferative effect on nine of ten soft-tissue sarcoma (STS) cell lines with IC50 values ranging in 0.025-5.9μM, with inhibition of the phosphorylation of Ser296 observed. GDC-0575 could synergy with gemcitabine. It abrogated DNA damage-induced S and G2–M checkpoints exacerbated DNA double-strand breaks and induced apoptosis in STS cells. Combined therapy of GDC-0575 (25mg/kg, orally) with gemcitabine twice a week for 3 weeks significantly reduced tumor growth increased progression-free survival of a P53mut UPS PDX model. GDC-0575 could enhance AraC-mediated killing of AML cells both in vitro and in vivo with abrogation of any potential chemoresistance mechanisms involving DNA repair.
作用机制 GDC-0575 is an ATP-competitive CHK1 inhibitor.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.22mL

2.64mL

1.32mL

26.44mL

5.29mL

2.64mL