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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FLT3-CCT241736
CCT241736

Chemical Structure : CCT241736

CAS No.: 1402709-93-6

CCT241736 (Mobinitinib, CCT-241736 )

货号: PC-24959Not For Human Use, Lab Use Only.

CCT241736 (Mobinitinib) is a potent, orally bioavailable dual FLT3/Aurora kinase inhibitor with binding Kd of 7.5/48/6.2/38/14 nM for Aurora-A/Aurora-B/FLT3 WT/FLT3-ITD/FLT3(D835Y) respectively.

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10 mg ¥780 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CCT241736 (Mobinitinib) is a potent, orally bioavailable dual FLT3/Aurora kinase inhibitor with binding Kd of 7.5/48/6.2/38/14 nM for Aurora-A/Aurora-B/FLT3 WT/FLT3-ITD/FLT3(D835Y) respectively.
CCT241736 (Mobinitinib) shows S(10) selectivity score of 0.057 in a 442-kinase panel (containing 386 nonmutant kinases) at a concentration of 1 μM using the KINOMEScan technology.
CCT241736 (Mobinitinib) displays antiproliferative activity in a range of human tumor cell lines, including HCT116 human colon carcinoma (GI50 = 0.300 μM) and the human FLT3-ITD positive AML cell lines MOLM-13 (GI50 = 0.104 μM) and MV4–11 (GI50 = 0.291 μM). inhibited both the autophosphorylation of Aurora-A at T288 (a biomarker for Aurora-A inhibition: IC50 = 0.030 μM) and histone H3 phosphorylation at S10 (a biomarker for Aurora-B inhibition: IC50 = 0.148 μM) in HeLa cells.
CCT241736 (Mobinitinib) (50-100 mg/kg po b.i.d.) significantly inhibits the growth of MV4–11 human FLT3-ITD positive AML tumor xenografts in athymic mice.

物理化学性质&存储条件

分子量 456.38
分子式 C22H23Cl2N7
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-Chloro-7-(4-(4-chlorobenzyl)piperazin-1-yl)-2-(1,3-dimethyl-1H-pyrazol-4-yl)-1H-imidazo[4,5-b]pyridine

参考文献

1. Wood FL, et al. Eur J Pharm Sci. 2019 Nov 1;139:104899.

2. Bavetsias V, et al. J Med Chem. 2012 Oct 25;55(20):8721-34.

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