Shanghai Nianxing Industrial Co., Ltd
China
Product Name: GDC-0575
Price:
Purity: 98.0%
Stocking Period: 10 Day
Contact: Yang

ShangHai DC Chemicals Co.,Ltd
China
Product Name: GDC-0575
Price: ￥Inquiry/1g
Purity: 98.9%
Stocking Period: 1 Day
Contact: Tony Lai

DC Chemicals Limited
China
Product Name: GDC-0575
Price: $600.0/100mg $1100.0/250mg $2200.0/1g
Purity: 98.0%
Stocking Period: 1 Day
Contact: Tony Cao

1196504-54-7

1196504-54-7 structure

1196504-54-7 structure

Name: GDC-0575
Chemical Name: GDC-0575
CAS Number: 1196504-54-7
Molecular Formula: C₁₆H₂₁BrClN₅O
Molecular Weight: 414.73
Create Date: 2020-04-12 11:34:15
Modify Date: 2024-04-05 14:48:12
GDC0575 (ARRY-575) hydrochloride is a highly-selective and orally active Chk1 (IC50=1.2 nM) inhibitor. GDC0575 (ARRY-575) hydrochloride can be used for colitis-associated cancer (CAC) and colitis research[1].

Name	GDC-0575

Description	GDC0575 (ARRY-575) hydrochloride is a highly-selective and orally active Chk1 (IC50=1.2 nM) inhibitor. GDC0575 (ARRY-575) hydrochloride can be used for colitis-associated cancer (CAC) and colitis research[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> Checkpoint Kinase (Chk) Research Areas >> Inflammation/Immunology
Target	Chk1:1.2 nM (IC50)
In Vitro	GDC-0575 dihydrochloride 是一种选择性的具有口服活性的 CHK1 抑制剂，IC50为 1.2 nM。GDC-0575 (100 nM) 通过降低 tyr15 磷酸化 CDK2 水平抑制 AraC 诱导的 CHK1 激活[1]. GDC-0575 dihydrochloride (100 nM) 对 AML 细胞活力无影响，但与 AraC 联合使用可显著降低细胞活力，诱导细胞凋亡。GDC-0575 dihydrochloride 加 AraC 对正常造血干细胞 (HSPCs) 无影响[1]。GDC-0575 dihydrochloride 对 20 种黑色素瘤细胞系显示出细胞毒活性，但一些作为肿瘤球 (TS) 生长的细胞系相对不敏感[2]。
In Vivo	GDC-0575 dihydrochloride (7.5 mg/kg, p.o.) 联合 AraC 几乎可以完全消除移植 U937-Luc 细胞小鼠的白血病负担，并且比单独使用 AraC 更有效。GDC-0575 dihydrochloride 在体内不同原发性 AML 模型中提高 AraC 的细胞毒性[1]. GDC-0575 dihydrochloride (25、50 mg/kg, p.o.) 对 D20 和 C002 异种移植物肿瘤生长的剂量依赖性抑制作用[2].
References	[1]. Oo ZY, et al. Endogenous Replication Stress Marks Melanomas Sensitive to CHEK1 Inhibitors In Vivo. Clin Cancer Res. 2018 Mar 13. [2]. Laroche-Clary A, et al. CHK1 inhibition in soft-tissue sarcomas: biological and clinical implications. Ann Oncol. 2018 Apr 1;29(4):1023-1029. [3]. Di Tullio A, et al. The combination of CHK1 inhibitor with G-CSF overrides cytarabine resistance in human acute myeloid leukemia. Nat Commun. 2017 Nov 22;8(1):1679.

Molecular Formula	C₁₆H₂₁BrClN₅O
Molecular Weight	414.73
Storage condition	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO