GDC0575 hydrochloride  (Synonyms: ARRY-575 hydrochloride; RG7741 hydrochloride)

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].

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]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

414.73

C₁₆H₂₁BrClN₅O

1196504-54-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Oo ZY, et al. Endogenous Replication Stress Marks Melanomas Sensitive to CHEK1 Inhibitors In Vivo. Clin Cancer Res. 2018 Mar 13.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]