M4205 (IDRX-42)

Chemical Structure : M4205

CAS No.: 2590556-80-0

加入收藏

货号: PC-20159Not For Human Use, Lab Use Only.

M4205 (IDRX-42) is a potent, highly selective inhibitor of KIT mutations with cell IC50 of 52 nM on cKIT autophosphorylation in the GIST430/654 cell line.

规格	价格	库存
5 mg	￥1580	In stock
10 mg	￥2480	In stock
25 mg	￥4280	In stock
50 mg	￥7280	In stock
100 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

M4205 (IDRX-42) is a potent, highly selective inhibitor of KIT mutations with cell IC50 of 52 nM on cKIT autophosphorylation in the GIST430/654 cell line.
M4205 inhibits KIT autophosphorylation at Y703 in the imatinib sensitive GIST430 cell line with an IC50 value of 4 nM.
M4205 inhibits the imatinib-resistant cell line GIST430/654 (exon 11 and exon 13 mutation) and the AML cell line Kasumi-1 (exon 17 mutation N822 K) with IC50 values of 48 and 4 nM, respectively.
M4205 displays high selectivity in a biochemical panel of 398 kinases at 1uM, only inhibits PDGFRA, PDGFRB, KIT (wt), FLT3, CSF1R, and lymphocyte-specific protein tyrosine kinase (LCK) with >80% inhibtion.
M4205 also displays high cellular kinase selectivity at 1 μM using a panel of NanoBRET assays, only bindsto KIT (wt) and FLT3 with 65% and 45% occupancy.
M4205 (35 mg/kg) showed strong in vivo tumor growth inhibition and led to regression in mice bearing GIST430/654 tumor, with dose- and exposure-dependent inhibition of KIT autophosphorylation.

物理化学性质&存储条件

分子量	508.63
分子式	C29H32N8O
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	N-(4-(1-methyl-1H-pyrazol-4-yl)benzyl)-6-(7-(3-(pyrrolidin-1-yl)propoxy)imidazo[1,2-a]pyridin-3-yl)pyrimidin-4-amine

参考文献

1. Andreas Blum, et al. J Med Chem. 2023 Feb 23;66(4):2386-2395.

M4205 (IDRX-42)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

M4205 (IDRX-42)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Get Quotation Now

* Indicates a Required FieldYour information is safe with us.