| Identification | Back Directory | [Name]
DS-1001b | [CAS]
1898206-17-1 | [Synonyms]
AB-218
DS-1001
Safusidenib
2-Propenoic acid, 3-[1-[[5-(1-fluoro-1-methylethyl)-3-(2,4,6-trichlorophenyl)-4-isoxazolyl]carbonyl]-3-methyl-1H-indol-4-yl]-, (2E)- | [Molecular Formula]
C25H18Cl3FN2O4 | [MOL File]
1898206-17-1.mol | [Molecular Weight]
535.78 |
| Hazard Information | Back Directory | [Uses]
Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma[1]. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively[2]. | [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[1]. | Animal Model: | NOD-SCID bearing JJ012 xenograft[3] | | Dosage: | Mixed with sterilized pellet food (CRF-1; Oriental Yeast) and fed ad libitum for 6 weeks.
Mixed with sterilized pellet food (CRF-1; Oriental Yeast) and fed ad libitum for 6 weeks. | | Administration: | Fed continuously starting at 3 weeks | | Result: | Continuous administration significantly impaired tumor growth in JJ012 xenograft mice. |
| [IC 50]
IDH1 | [References]
[1] Makoto Nakagawa, et al. Selective inhibition of mutant IDH1 by DS-1001b ameliorates aberrant histone modifications and impairs tumor activity in chondrosarcoma. Oncogene. 2019 Oct;38(42):6835-6849. DOI:10.1038/s41388-019-0929-9
[2] Yukino Machida, et al. A Potent Blood-Brain Barrier-Permeable Mutant IDH1 Inhibitor Suppresses the Growth of Glioblastoma with IDH1 Mutation in a Patient-Derived Orthotopic Xenograft Model. Mol Cancer Ther. 2020 Feb;19(2):375-383. DOI:10.1158/1535-7163.MCT-18-1349 |
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