产品
编 号：F747785
分子式：C25H18Cl3FN2O4
分子量：535.78
分子式：C25H18Cl3FN2O4
分子量：535.78
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CAS No: 1898206-17-1
产品详情
生物活性：
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. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively.
体内研究：
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.Animal Model:NOD-SCID bearing JJ012 xenograft
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.
体外研究：
Safusidenib (DS-1001b) impairs the proliferation of IDH1-mutated chondrosarcoma cell lines and decreases 2-HG levels.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.Safusidenib (1, and 10?μM; for 6 weeks) markedly upregulates SOX9, a key regulator of chondrocyte differentiation, at the protein level.Safusidenib (1 μM) significantly upregulates CDKN1C at the protein level.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.
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. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively.
体内研究：
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.Animal Model:NOD-SCID bearing JJ012 xenograft
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.
体外研究：
Safusidenib (DS-1001b) impairs the proliferation of IDH1-mutated chondrosarcoma cell lines and decreases 2-HG levels.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.Safusidenib (1, and 10?μM; for 6 weeks) markedly upregulates SOX9, a key regulator of chondrocyte differentiation, at the protein level.Safusidenib (1 μM) significantly upregulates CDKN1C at the protein level.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.
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