Flavopiridol HCl

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Chemical Structure| 131740-09-5 同义名 : HMR-1275 Hydrochloride; L86-8275 Hydrochloride; L-868,275; HL 275; Flavopiridol (hydrochloride); DSP-2033; HMR-1275; Alvocidib; NSC 649890; Alvocidib Hydrochloride; Flavopiridol Hydrochloride
CAS号 : 131740-09-5
货号 : A180731
分子式 : C21H21Cl2NO5
纯度 : 99%+
分子量 : 438.3
MDL号 : MFCD26792554
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

PO 0.5% CMC-Na 50 mg/mL suspension

生物活性
描述 At a concentration of 2 μM, Flavopiridol significantly triggers ER stress in CLL cells, leading to cell death via the activation of IRE1, ASK1, and potentially downstream caspases[1]. Flavopiridol causes a strong increase in the expression of various PRGs over 4-24 hours of treatment. It has both immediate and prolonged effects on PRG expression levels. Even in serum-deprived cells that are later re-exposed to serum, Flavopiridol suppresses gene expression initially, but later, genes such as JUNB, GADD45B, and EGR1 experience an upsurge in their expression due to Flavopiridol[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
A2780 cell Function assay Inhibition of A2780 cell clonogenic assay， IC50=15 μM 11063609
A2780/DDP-R human ovarian carcinoma cell Proliferation assay Inhibition of A2780/DDP-R human ovarian carcinoma cell proliferation, IC50=38 nM 12190313
A2780/DDP-S human ovarian carcinoma cell Proliferation assay Inhibition of A2780/DDP-S human ovarian carcinoma cell proliferation, IC50=56 nM 12190313
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02520011 Acute Myeloid Leukemia Phase 2 Recruiting December 2019 -
NCT00006485 Unspecified Adult Solid Tumor,... 展开 >> Protocol Specific 收起 << Phase 1 Completed - United States, New York ... 展开 >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 收起 <<
NCT00087282 Liver Cancer Phase 2 Completed - United States, New York ... 展开 >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.28mL

0.46mL

0.23mL

11.41mL

2.28mL

1.14mL

22.82mL

4.56mL

2.28mL
参考文献

[1]Senderowicz AM. The cell cycle as a target for cancer therapy: basic and clinical findings with the small molecule inhibitors flavopiridol and UCN-01. Oncologist. 2002;7 Suppl 3:12-9.

[2]Carlson BA, Dubay MM, et al. Flavopiridol induces G1 arrest with inhibition of cyclin-dependent kinase (CDK) 2 and CDK4 in human breast carcinoma cells. Cancer Res. 1996 Jul 1;56(13):2973-8.