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Chemical Structure : M4205
CAS No.: 2590556-80-0
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $158 | In stock | |
| 10 mg | $248 | In stock | |
| 25 mg | $428 | In stock | |
| 50 mg | $728 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 508.63 | |
| Formula | C29H32N8O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Andreas Blum, et al. J Med Chem. 2023 Feb 23;66(4):2386-2395.
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