SAR020106

产品编号: DC9792 Featured
SAR020106
结构式
1184843-57-9
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中国地区超过5000个高品质化合物库存
应用领域
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme.
Cas No.: 1184843-57-9
名称:
别名: SAR020106; SAR020106; SAR 020106; SAR20106; SAR20106; SAR 20106
SMILES: C1(C2=C(C=C(N=C2)NC2C=NC(C#N)=C(O[C@@H](CN(C)C)C)N=2)C=CC=1)Cl
分子式: C19H19ClN6O
分子量: 382.13
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion. Biomarker studies have shown that SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion both in vitro and in vivo. SAR-020106 represents a novel class of CHK1 inhibitors that can enhance antitumor activity with selected anticancer drugs in vivo and may therefore have clinical utility.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
TITLE DOWNLOAD
MSDS_2801_DC9792_1184843-57-9
COA
LOT NO. DOWNLOAD
产品编号 产品名称 应用领域
DC9924 SB218078 SB-218078 是一种有效的,选择性,ATP 竞争性且细胞可渗透的检查点激酶 1 (Chk1) 抑制剂,可抑制 cdc25C 的 Chk1 磷酸化,IC50 为 15 nM。SB-218078 对 Cdc2 (IC50 为 250 nM) 和 PKC (IC50 为 1000 nM) 的抑制作用较弱。SB-218078 通过 DNA 损伤和细胞周期停滞诱导细胞凋亡。
DC9792 SAR020106 SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme.
DC8324 CCT244747 CCT244747 是一种有效的,可口服的,高度选择性的 CHK1 抑制剂,IC50 值为 7.7 nM;CCT244747 可废除 G2 检查点,IC50 值为 29 nM。