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CG'806(CG-806) 目录号:GY07333 新品

CAS号:1370466-81-1

分子式:C26H19F4N5O2

分子量:509.45

CG'806是新型的FLT3/BTK等多种激酶的抑制剂,旨在解决依鲁替尼的缺点。

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5mg 4388 咨询
10mg 6413 咨询
25mg 13163 咨询
50mg 19913 咨询
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产品仅用于科研,严禁用于临床

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生物活性实验指南文献化学信息溶解性

生物活性(数据来源于公开文献,仅供参考)

产品简述 CG'806是新型的FLT3/BTK等多种激酶的抑制剂,旨在解决依鲁替尼的缺点。
靶点 & IC50
FLT3/BTK [1]
细胞 & 酶实验结果 CG-806 (CG'806) is a small molecule multi-kinase inhibitor against FLT3 and BTK kinases that is under development to treat FLT3-driven AML. CG-806 exerts potent picomolar IC50 anti-proliferative activity against human AML cells and against Ba/F3 mouse AML cells with FLT3-ITD mutations (about 50 to 250-fold higher activity compared to quizartinib or gilteritinib). Specifically, compared to second-generation FLT3 inhibitors quizartinib or gilteritinib, CG-806 shows much more pronounced anti-proliferative effects in leukemia cells with D835 mutations, the ITD plus F691L/Y842D/D835 mutations, or in FLT3 wild-type cells (IC50s are 0.17, 0.82, 9.49, 0.30, 8.26, 9.72, and 0.43 nM for human ITD-mutated AML cells MV4-11, MOLM13, murine ITD mutated leukemia cells Ba/F3 WT, Ba/F3-ITD, Ba/F3-D835Y, Ba/FLT3-ITD+D835Y, and “gatekeeper” mutation Ba/F3-ITD+F691L cells, respectively). Furthermore, CG-8066 triggers profound apoptosis in cell lines. Mechanistically, CG-806 profoundly suppresses FLT3 and its downstream MAPK/AKT signaling, as well as phospho-Aurora, and/or phospho-BTK proteins, suggesting the ability of CG-806 to inhibit various kinases that function in AML signaling and appear to contribute to its effectiveness[1].
动物实验结果 CG-806 demonstrates in vivo tumor eradication without toxicity when administered orally, once daily for 14 d as a single agent in the MV4:11 AML murine xenograft model, and demonstrates sustained micromolar plasma drug levels in mice after a single oral administration. CG-806 can be considered not only a pan-FLT3 inhibitor for targeting FLT3 wild type and ITD-mutant AML, but also a one-of-a-kind agent killing leukemia cells with TKD or dual TKD plus ITD mutations, which are frequently associated with resistance/relapse in FLT3-mutant AML patients. CG-806 exerts a robust therapeutic window in animal xenograft studies. Thus, CG-806 warrants further investigation for the treatment of newly diagnosed and relapsed/refractory patients with FLT3-mutated AML[1].

实验指南

激酶实验
细胞实验:
细胞株
浓度
孵化时间
实验方法
动物实验:
动物模型
剂型
剂量
给药方式

化学信息

CAS号 1370466-81-1
分子式 C26H19F4N5O2
分子量 509.45
稳定性 粉末,-20°C,2年;DMSO溶剂,4°C,2周;DMSO溶剂,-80°C,6个月

溶解性(仅供参考)

体内实验溶剂
动物实验剂型
由于生产工艺和批次不同,溶解性可能会有所差异。

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