DS-1001b
- CAS No.
- 1898206-17-1
- Chemical Name:
- DS-1001b
- 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)-
- CBNumber:
- CB18941289
- Molecular Formula:
- C25H18Cl3FN2O4
- Molecular Weight:
- 535.78
- MDL Number:
- MOL File:
- 1898206-17-1.mol
Boiling point | 651.9±55.0 °C(Predicted) |
---|---|
Density | 1.45±0.1 g/cm3(Predicted) |
pka | 4.37±0.40(Predicted) |
FDA UNII | RCK8KK7SB9 |
DS-1001b Chemical Properties,Uses,Production
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
DS-1001b Preparation Products And Raw materials
Raw materials
Preparation Products
DS-1001b Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +17819995354 | marketing@targetmol.com | United States | 19903 | 58 |
Kaixin Chemical (Hong Kong) Limited | 010-88886666-01 13112345678 | loyson@tcypharm.com | China | 596 | 55 |
Jinan Kabotang Biological Technology Co.,Ltd. | 0531-61320525 15866703830 | figo.gao@foxmail.com | China | 4561 | 58 |
mahaloong | +86-028-81192082 +86-18180560816 | sales@mahaloong.com | China | 595 | 58 |
TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 20622 | 58 |
Supplier | Advantage |
---|---|
TargetMol Chemicals Inc. | 58 |
Kaixin Chemical (Hong Kong) Limited | 55 |
Jinan Kabotang Biological Technology Co.,Ltd. | 58 |
mahaloong | 58 |
TargetMol Chemicals Inc. | 58 |
View Lastest Price from DS-1001b manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
![]() |
2025-04-28 | Safusidenib
1898206-17-1
|
US $2500.00-1520.00 / mg | 10g | TargetMol Chemicals Inc. |
-
- Safusidenib
1898206-17-1
- US $2500.00-1520.00 / mg
- TargetMol Chemicals Inc.