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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-p97/VCP-CB5339
CB5339

Chemical Structure : CB5339

CAS No.: 1863952-15-1

CB5339 (CB-5339, CB 5339)

货号: PC-72409Not For Human Use, Lab Use Only.

CB5339 (CB-5339) is a second-generation, potent, selective, ATP-competitive, and oral inhibitor of valosin-containing protein (VCP/p97) with IC50 of 9 nM.

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10 mg ¥2180 In stock
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50 mg ¥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CB5339 (CB-5339) is a second-generation, potent, selective, ATP-competitive, and oral inhibitor of valosin-containing protein (VCP/p97) with IC50 of 9 nM.
CB-5339 was 15-fold less active on the human cone PDE6 (PDE6C, IC50=3900 nM) in in vitro biochemical assays, and displayed a 31-times lower Cmax in vivo in rat retina compared to CB-5083.
CB5339 demonstrated growth inhibition against a panel of 16 AML cell lines and a panel of 16 primary AML patient samples harboring diverse genetic backgrounds (mean IC50 =375 nM).
CB5339 was validated in multiple AML models, including syngeneic and patient-derived xenograft murine models.
CB-5339 treatment synergizes to impair leukemic growth in an MLL-AF9-driven AML murine model when combined with DNA-damaging agents anthracyclines.

物理化学性质&存储条件

分子量 412.497
分子式 C24H24N6O
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

1-(4-(benzylamino)-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxamide

参考文献

1. Blandine Roux, et al. Sci Transl Med. 2021 Mar 31;13(587):eabg1168.

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