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CAS No.: 1402709-93-6

CCT241736 Catalog No. CSN27200

Synonyms: CCT241736

CCT241736 is a dual FLT3/Aurora kinase A/B inhibitor with IC50 values of 0.035μM, 0.015μM and 0.1μM, respectively.

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技术信息

生物活性

描述Aurora kinases, a family of three serine-threonine kinases designated A, B, and C, play key and distinct roles in different stages of mitosis. CCT241736 is a potent and orally bioavailable dual FLT3/Aurora kinase inhibitor with K_d values of 7.5, 48, 6.2, 38 and 14 nM for Aurora-A, Aurora-B, FLT3 kinase and FLT3 mutants FLT3-ITD and FLT3(D835Y), respectively. In addition, CCT241736 inhibited Aurora-A with an IC₅₀ value of 0.038 μM. CCT241736 inhibited the SW620 tumor cell growth with GI₅₀ value of 0.283 μM. CCT241736 displayed antiproliferative activity in HCT116 human colon carcinoma (GI₅₀ = 0.3 μM) and the human FLT3-ITD positive AML cell lines MOLM-13 (GI₅₀ = 0.104 μM) and MV4−11 (GI₅₀ = 0.291 μM). In Hela cervical cancer cells, CCT241736 inhibited both the autophosphorylation of Aurora-A at T288 (a biomarker for Aurora-A inhibition: IC₅₀ = 0.03 μM) and histone H3 phosphorylation at S10 (a biomarker for Aurora-B inhibition: IC₅₀ = 0.148 μM). In an in vivo setting, CCT241736 strongly inhibited the growth of a FLT3-ITD-positive acute myeloid leukemia (AML) human tumor xenograft (MV4-11) in a dose-dependent manner following oral administration^[2].
参考文献

[1] Moore AS, Faisal A, Mak GWY, et al. Quizartinib-resistant FLT3-ITD acute myeloid leukemia cells are sensitive to the FLT3-Aurora kinase inhibitor CCT241736. Blood Adv. 2020;4(7):1478-1491. doi:10.1182/bloodadvances.2019000986
[2] Bavetsias V, Crumpler S, et al. Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. J Med Chem. 2012 Oct 25;55(20):8721-34.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1912 mL
- 10.9560 mL
- 21.9120 mL
- 5 mM
- 0.4382 mL
- 2.1912 mL
- 4.3824 mL
- 10 mM
- 0.2191 mL
- 1.0956 mL
- 2.1912 mL

技术信息

CAS号

1402709-93-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H23Cl2N7

运输

蓝冰

分子量

456.37

别名

CCT241736

溶解度

DMSO	73.0 mg/mL (160.0 mM) warming
Water	Insoluble

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