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Chemical Structure : DS-1001b
CAS No.: 1898207-64-1
Catalog No.: PC-38189Not For Human Use, Lab Use Only.
DS-1001b (DS1001b) is a potent, selective, BBB-permeable and orally bioavailable mutant IDH1 inhibitor with IC50 of 8.4/11 nM against IDH1 R132H/R132C mutants.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $118 | In stock | |
| 25 mg | $198 | In stock | |
| 50 mg | $328 | In stock | |
| 100 mg | Get quote |
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DS-1001b (DS1001b, Safusidenib) is a potent, selective, BBB-permeable and orally bioavailable mutant IDH1 inhibitor with IC50 of 8.4/11 nM against IDH1 R132H/R132C mutants.
DS-1001b strongly inhibited mutant IDH1, but not wild-type IDH1 or mutant IDH2 (IC50>10 uM).
DS-1001b impairs the proliferation of IDH1 mutant GBM cells and induces differentiation in a subcutaneous PDX model, but not the growth of IDH wild-type GBM.
DS-1001b permeates the BBB and inhibits tumor growth in an orthotopic PDX model.
| M.Wt | 608.916 | |
| Formula | C29H29Cl3FN3O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-methylpropan-2-amine (E)-3-(1-(5-(2-fluoropropan-2-yl)-3-(2,4,6-trichlorophenyl)isoxazole-4-carbonyl)-3-methyl-1H-indol-4-yl)acrylate |
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1. Yukino Machida, et al. Mol Cancer Ther. 2020 Feb;19(2):375-383.
2. Nakagawa M, et al. Oncogene. 2019 Oct;38(42):6835-6849.
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