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- 2025年07月15日
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- 详细信息
- 技术资料
- 保存条件：
4°C, sealed storage, away from moisture
- 英文名：
ARRY-575 dihydrochloride; RG7741 dihydrochloride
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1657014-42-0
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2090.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥1900.0 |
| 规格： | 10 mg | 产品价格： | ￥3000.0 |
| 规格： | 25 mg | 产品价格： | ￥5200.0 |
| 规格： | 50 mg | 产品价格： | ￥7800.0 |
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GDC-0575 dihydrochloride
CAS No. : 1657014-42-0
MCE 国际站：GDC-0575 dihydrochloride
产品活性：GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) 是一种选择性的，可口服的 CHK1 抑制剂，IC50 值为 1.2 nM，具有抗肿瘤活性。
研究领域：Cell Cycle/DNA Damage
作用靶点：Checkpoint Kinase (Chk)
In Vitro: GDC-0575 dihydrochloride is a selective and orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM. GDC-0575 (100 nM) suppressses CHK1 activation induced by AraC by decreasing the level of Tyr15-phosphorylated CDK2. GDC-0575 (100 nM) has no effect on the viability of AML cells, but significantly reduces cell viability and induces apoptosis in combination with AraC. In addition, GDC-0575 plus AraC shows no effect on normal hematopoietic stem and progenitor cells (HSPCs). GDC-0575 shows cytotoxic activity against most of 20 melanoma cell lines tested, but several cell lines grown as tumour sphere (TS) are relatively insensitive.
In Vivo: GDC-0575 (7.5 mg/kg, p.o.) in combination with AraC alomost completely eradicates leukemic burden in mice transplanted with U937-Luc cells, and shows more efficient activity than AraC alone. Furthermore, GDC-0575 elevates the cytotoxicity of AraC in different primary AML models in vivo. GDC-0575 (25, 50 mg/kg, p.o.) dose-dependently inhibits the growth of tumor in D20 and C002 xenografts.
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