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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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Mutant IDH1-IN-4
Mutant IDH1-IN-4 is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH 1) with an IC50 value of ≤ 0.5 μM for mutant IDH 1 in R132H, HT1080 and U87R132H cells. |
(S,S)-GSK321
(S,S)-GSK321 is the (S,S)-enantiomer of GSK321.GSK321 is a potent inhibitor of the mutant isocitrate dehydrogenase 1 (IDH1) enzyme. |
IDH1 Inhibitor 1
IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-permeable, selective mutant IDH1 inhibitor that inhibits IDH1R132H, IDH1R132C, and IDH1WT with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM, respectively. possesses antitumor activity. |
IDH1 Inhibitor 7
IDH1 Inhibitor 7 is an IDH1 inhibitor with an IC50 of less than 100 nM. |
(R,R)-GSK321
(R,R)-GSK321 is an isomer of GSK321 and a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. |
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