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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-FHD-286
FHD-286

Chemical Structure : FHD-286

CAS No.: 2671128-05-3

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FHD-286 (FHD286, Camibirstat)

货号: PC-73320Not For Human Use, Lab Use Only.

Camibirstat (FHD-286) is a highly potent, selective, allosteric and orally available inhibitor of BRM (SMARCA2) and BRG1 (SMARCA4) ATPase subunits with IC50 of 4.5 nM and 6.5 nM, respectively.

规格 价格 库存 数量
1 mg ￥1580 In stock
5 mg ￥2980 In stock
10 mg ￥4780 In stock
25 mg ￥7280 In stock
50 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Camibirstat (FHD-286) is a highly potent, selective, allosteric and orally available inhibitor of BRM (SMARCA2) and BRG1 (SMARCA4) ATPase subunits with IC50 of 4.5 nM and 6.5 nM, respectively.
FHD-286 showed low nanomolar activity in cellular MMTV luciferase assays and potent antitumor activity against the uveal melanoma 92-1 cell line both in vitro and in vivo in a mouse xenograft model.
FHD-286 has shown antiproliferative activity in xenograft models of non-small-cell lung cancer and prostate cancer.
FHD-286 has also been reported to resensitize TKI-resistant lung cancer to an EGFR inhibitor and tumor growth inhibition was observed when the two inhibitors were treated in combination in a patient-derived mouse xenograft model.

物理化学性质&存储条件

分子量 562.660
分子式 C24H30N6O6S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-((S)-1-((4-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-2-yl)thiazol-2-yl)amino)-3-methoxy-1-oxopropan-2-yl)-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide

参考文献

1. Warren C. Fiskus, et al. Cancer Res (2023) 83 (7_Supplement): 1140.
2. Fiskus W, et al. Blood. 2024 May 16;143(20):2059-2072.

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