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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-CUDC-907
CUDC-907

Chemical Structure : CUDC-907

CAS No.: 1339928-25-4

CUDC-907 (Fimepinostat, CUDC907)

货号: PC-49141Not For Human Use, Lab Use Only.

Fimepinostat (CUDC-907) is a potent, dual-acting PI3K and HDAC inhibitor, potently inhibits HDAC classes I and II enzymes, inhibits class I PI3K kinases with IC50 of 19, 54, and 39 nM for PI3Kα, PI3Kβ, and PI3Kδ, respectively.

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5 mg ¥780 In stock
10 mg ¥1180 In stock
50 mg ¥2880 In stock
100 mg ¥4780 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

Fimepinostat (CUDC-907) is a potent, dual-acting PI3K and HDAC inhibitor, potently inhibits HDAC classes I and II enzymes, inhibits class I PI3K kinases with IC50 of 19, 54, and 39 nM for PI3Kα, PI3Kβ, and PI3Kδ, respectively.
CUDC-907 inhibitsthe PI3K pathway, as indicated by the dose-dependent decreases in phosphorylation of AKT and its downstream targets, 4EBP-1 and p70S6, in H460 cells.
CUDC-907 durably suppresses activation of AKT and modulates receptor tyrosine kinase, RAF-MEK-MAPK and SRC/STAT signaling via HDAC inhibition, downregulates and suppresses the activation of the SRC/STAT signaling pathway and multiple receptor tyrosine kinases.
CUDC-907 induces apoptosis and G2-M cell-cycle arrest in cancer cells, and effectively inhibits cancer cell growth (MOLT4 cell, IC50=1 nM).
CUDC-907 (25, 50, and 100 mg/kg, oral) suppresses tumor growth, inhibits HDAC activity, and blocks signaling of PI3K and MAPK pathways in xenograft models.
CUDC-907 (500 nM) exhibits enhanced adipocytic differentiation in human bone marrow stromal cells (hBMSCs).

物理化学性质&存储条件

分子量 508.557
分子式 C23H24N8O4S
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-hydroxy-2-[[[2-(6-methoxy-3-pyridinyl)-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]methylamino]-5-pyrimidinecarboxamide

参考文献

1. Qian C, et al. Clin Cancer Res. 2012 Aug 1;18(15):4104-13.

2. Sun K, et al. Mol Cancer Ther. 2017 Feb;16(2):285-299.

3. Ali D, et al. Stem Cells Dev. 2017 Mar 1;26(5):353-362.

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