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Safusidenib
Safusidenib 是一种口服有效的选择性 IDH1突变型抑制剂。Safusidenib 强烈抑制突变型 IDH1 但不抑制野生型 IDH1。Safusidenib 会削弱软骨肉瘤中的肿瘤活性。Safusidenib 对 IDH1R132H 和 IDH1R132C 具有活性，在没有预孵育的情况下，IC50 分别为 15 和 130 nM。
Safusidenib Chemical Structure
CAS No. : 1898206-17-1
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
Safusidenib 的其他形式现货产品:
DS-1001b
| 生物活性 |
Safusidenib 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].
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体外研究
(In Vitro) |
Safusidenib (DS-1001b) impairs the proliferation of IDH1-mutated chondrosarcoma cell lines and decreases 2-HG levels[1].
Safusidenib impairs the proliferation of IDH1 mutant chondrosarcoma cell lines in a dose-dependent manner, whereas Safusidenib has little effect on the proliferation of the IDH wild-type cell lines OUMS27 and NDCS-1; GI50 values for JJ012, L835, OUMS27, and NDCS-1 cells are 81 nM (day 14), 77 nM (6 weeks), >10 μM (day 10), and >10 μM (day 10), respectively[1].
Safusidenib (1, and 10 μM; for 6 weeks) markedly upregulates SOX9, a key regulator of chondrocyte differentiation, at the protein level[1].
Safusidenib (1 μM) significantly upregulates CDKN1C at the protein level[1].
Safusidenib (DS-1001b) exhibits activity against IDH1 or IDH2 enzymes with IC50s of 8.4, 11, and 180 nM for IDH1R132H, IDH1R132C, and IDH1WT in assays conducted with a 2-hour preincubation step[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
| Cell Line: |
The IDH1 mutant cell lines JJ012 and L835 cells |
| Concentration: |
0.1, 1, and 10 μM |
| Incubation Time: |
0, 3, 6, 9, 12, and 15 days |
| Result: |
Impaired proliferation in both cell lines in a dose-dependent manner. |
Western Blot Analysis[1]
| Cell Line: |
L835 cells |
| Concentration: |
0, 1, and 10 μM |
| Incubation Time: |
6 weeks |
| Result: |
Markedly upregulated SOX9 at the protein level. |
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体内研究
(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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[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.
[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.
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