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DS-1001b (Safusidenib t-Butylamine) is a potent, orally bioavailable, selective mutant IDH-1 (Isocitrate Dehydrogenase-1) inhibitor with antitumor activity. DS-1001b (Safusidenib t-Butylamine) impairs the proliferation of IDH1 mutant chondrosarcoma cell lines and decreases 2-HG levels. DS-1001b exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively.
In vivo, Safusidenib (DS-1001b) has antineoplastic activity in JJ012 xenografts. Continuous administration of Safusidenib (mixed with sterilized pellet food and fed continuously for 6 weeks) impairs tumor growth in xenograft mice.
| Molecular Weight | 608.92 |
| Formula | C29H29Cl3FN3O4 |
| CAS Number | 1898207-64-1 |
| Solubility (25°C) | DMSO ≥ 18 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Isocitrate Dehydrogenase (IDH) Products |
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| AGI-5198
AGI-5198 (IDH-C35) is the first highly potent and selective inhibitor of IDH1 R132H and R132C mutants in vitro with IC50 values of 0.07 μM and 0.16 μM, respectively. |
| AGI-6780
AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM. |
| Enasidenib
Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively. |
| BAY-1436032
BAY1436032 is a novel pan-mutant IDH1 inhibitor, it specifically inhibits R-2HG production and colony growth, and induces myeloid differentiation of AML cells. |
| GSK864
GSK864 is a cell penetrant, potent and selective allosteric inhibitor of isocitrate dehydrogenase 1 (IDH1) that potently inhibits intracellular 2-hydroxyglutarate (2-HG) production in HT-1080 cells. |
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