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DS-1001

Chemical Structure : DS-1001

CAS No.: 1898206-17-1

DS-1001 (DS1001, Safusidenib)

Catalog No.: PC-38188Not For Human Use, Lab Use Only.

DS-1001 (DS1001, 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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

DS-1001 (DS1001, 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.

Physicochemical Properties

M.Wt 535.777
Formula C25H18Cl3FN2O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(E)-3-(1-(5-(2-fluoropropan-2-yl)-3-(2,4,6-trichlorophenyl)isoxazole-4-carbonyl)-3-methyl-1H-indol-4-yl)acrylic acid

References

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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