CCT244747

产品编号: DC8324 Featured
CCT244747
结构式
1404095-34-6
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中国地区超过5000个高品质化合物库存
应用领域
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。
Cas No.: 1404095-34-6
名称: 3-((1-(dimethylamino)propan-2-yl)oxy)-5-((4-methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)amino)pyrazine-2-carbonitrile
别名: CCT244747; CCT-244747; CCT 244747
SMILES: N1C=C(NC2N=CC(C3C=NN(C)C=3)=C(OC)C=2)N=C(O[C@@H](CN(C)C)C)C=1C#N
分子式: C20H24N8O2
分子量: 408.46
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: CCT244747 inhibited cellular CHK1 activity (IC(50) 29-170 nmol/L), significantly enhanced the cytotoxicity of several anticancer drugs, and abrogated drug-induced S and G(2) arrest in multiple tumor cell lines. Biomarkers of CHK1 (pS296 CHK1) activity and cell-cycle inactivity (pY15 CDK1) were induced by genotoxics and inhibited by CCT244747 both in vitro and in vivo, producing enhanced DNA damage and apoptosis. Active tumor concentrations of CCT244747 were obtained following oral administration. The antitumor activity of both gemcitabine and irinotecan were significantly enhanced by CCT244747 in several human tumor xenografts, giving concomitant biomarker modulation indicative of CHK1 inhibition. CCT244747 also showed marked antitumor activity as a single agent in a MYCN-driven neuroblastoma. For the detailed information of CCT244747, the solubility of CCT244747 in water, the solubility of CCT244747 in DMSO, the solubility of CCT244747 in PBS buffer, the animal experiment (test) of CCT244747, the cell expriment (test) of CCT244747, the in vivo, in vitro and clinical trial test of CCT244747, the EC50, IC50,and affinity,of CCT244747, For the detailed information of CCT244747, the solubility of CCT244747 in water, the solubility of CCT244747 in DMSO, the solubility of CCT244747 in PBS buffer, the animal experiment (test) of CCT244747, the cell expriment (test) of CCT244747, the in vivo, in vitro and clinical trial test of CCT244747, the EC50, IC50,and affinity,of CCT244747, Please contact DC Chemicals.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
TITLE DOWNLOAD
MSDS_2272_DC8324_1404095-34-6
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。