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首页-小分子抑制剂&激动剂-Tyrosine Kinase-c-Kit-Amuvatinib
Amuvatinib

Chemical Structure : Amuvatinib

CAS No.: 850879-09-3

Amuvatinib (MP-470;MP 470;MP470;HPK-56;HPK56)

货号: PC-42451Not For Human Use, Lab Use Only.

Amuvatinib (MP-470) is a potent RTK inhibitor that effectively inhibits c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Amuvatinib (MP-470) is a potent RTK inhibitor that effectively inhibits c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively.
Amuvatinib (MP-470) also inhibits several mutants of c-Kit and Axl.
Amuvatinib (MP-470) inhibits prostate cancer cell proliferation (IC50=4-8 uM), promotes cell cycle arrest and apoptosis.
Amuvatinib (MP-470) completely inhibites phosphorylation of the HER members (HER1, 2, 3), binding of PI3K regulatory unit p85 to HER3 and downstream Akt activity in combination with Erlotinib.
Amuvatinib (MP-470) exhibits synergistic effect in LNCaP mouse xenograft model.

物理化学性质&存储条件

分子量 447.5096
分子式 C23H21N5O3S
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

1-Piperazinecarbothioamide, N-(1,3-benzodioxol-5-ylmethyl)-4-benzofuro[3,2-d]pyrimidin-4-yl-

参考文献

1. Mahadevan D, et al. Oncogene. 2007 Jun 7;26(27):3909-19.

2. Qi W, et al. BMC Cancer. 2009 May 11;9:142.

4. Bearss DJ, et al. US Patent, US/2008/0226747.

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