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Flavopiridol HCl {[allProObj[0].p_purity_real_show]}

货号:A180731 同义名: HMR-1275 Hydrochloride; L86-8275 Hydrochloride

Flavopiridol HCl competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM.

Flavopiridol HCl 化学结构 CAS号:131740-09-5
Flavopiridol HCl 化学结构
CAS号:131740-09-5
Flavopiridol HCl 3D分子结构
CAS号:131740-09-5
Flavopiridol HCl 化学结构 CAS号:131740-09-5
Flavopiridol HCl 3D分子结构 CAS号:131740-09-5
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Flavopiridol HCl 纯度/质量文件 产品仅供科研

货号:A180731 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

全球学术期刊中引用的产品

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产品名称 Cdc CDK1 CDK19 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CLK 其他靶点 纯度
XL413 HCl ++++

Cdc7, IC50: 3.4 nM

99%+
SU9516 +++

CDK1, IC50: 40 nM

+++

CDK2, IC50: 22 nM

++

CDK4, IC50: 200 nM

99%+
RO-3306 +++

CDK1, Ki: 20 nM

ERK,SGK 98%
R547 ++++

CDK1/CyclinB, Ki: 2 nM

++++

CDK2/CyclinE, Ki: 3 nM

++++

CDK4/CyclinD1, Ki: 1 nM

99%+
BMS-265246 ++++

CDK1/CyclinB, IC50: 6 nM

++++

CDK2/CyclinE, IC50: 9 nM

+

CDK4/CyclinD, IC50: 230 nM

99%+
NU6027 +

CDK1, Ki: 2.5 μM

+

CDK2, Ki: 1.3 μM

DNA-PK 98%
Purvalanol A ++++

Cdc2/CyclinB, IC50: 4 nM

+++

CDK2/CyclinE, IC50: 35 nM

CDK2/CyclinA, IC50: 70 nM

+

CDK4/CyclinD1, IC50: 850 nM

99%+
SCH900776 ++

CDK2, IC50: 0.16 μM

99%+
AUZ 454 ++++

CDK2(A144C), Kd: 9.7 nM

CDK2(C118L), Kd: 18.6 nM

99%+
A-674563 HCl ++

CDK2, Ki: 46 nM

PKA 99%
JNJ-7706621 ++++

CDK1/CyclinB, IC50: 9 nM

++++

CDK2/CyclinE, IC50: 3 nM

CDK2/CyclinA, IC50: 4 nM

++

CDK3/CyclinE, IC50: 58 nM

+

CDK4/CyclinD1, IC50: 253 nM

++

CDK6/CyclinD1, IC50: 175 nM

99%+
AT7519 ++

CDK1/CyclinB, IC50: 210 nM

++

CDK2/CyclinA, IC50: 47 nM

+

CDK3/CyclinE, IC50: 360 nM

++

CDK4/CyclinD1, IC50: 100 nM

+++

CDK5/p35, IC50: 13 nM

++

CDK6/CyclinD3, IC50: 170 nM

++++

CDK9/CyclinT, IC50: <10 nM

98+%
PHA-793887 ++

CDK1/CyclinB, IC50: 60 nM

++++

CDK2/CyclinE, IC50: 8 nM

CDK2/CyclinA, IC50: 8 nM

++

CDK4/CyclinD1, IC50: 62 nM

++++

CDK5/p25, IC50: 5 nM

++++

CDK7/CyclinH, IC50: 10 nM

++

CDK9/CyclinT1, IC50: 138 nM

99%+
Milciclib +

CDK1/CyclinB, IC50: 398 nM

++

CDK2/CyclinE, IC50: 363 nM

CDK2/CyclinA, IC50: 45 nM

++

CDK4/CyclinD1, IC50: 160 nM

+

CDK5/p35, IC50: 265 nM

++

CDK7/CyclinH, IC50: 150 nM

99%+
Kenpaullone +

CDK1/CyclinB, IC50: 0.4μM

+

CDK2/CyclinE, IC50: 7.5μM

CDK2/CyclinA, IC50: 0.68μM

+

CDK5/p35, IC50: 0.85μM

98%
SNS-032 +++

CDK2/CyclinE, IC50: 48 nM

CDK2/CyclinA, IC50: 38 nM

+

CDK5/p35, IC50: 340 nM

++

CDK7/CyclinH, IC50: 62 nM

++++

CDK9/CyclinT, IC50: 4 nM

99%+
Dinaciclib ++++

CDK1, IC50: 3 nM

++++

CDK2, IC50: 1 nM

++++

CDK5, IC50: 1 nM

++++

CDK9, IC50: 4 nM

99%+
PHA-767491 HCl ++++

Cdc7, IC50: 10 nM

+

CDK1, IC50: 250 nM

+

CDK2, IC50: 240 nM

+

CDK5, IC50: 460 nM

+++

CDK9, IC50: 34 nM

MK2 99%
(R)-Roscovitine +

Cdc2/CyclinB, IC50: 0.65 μM

+

CDK2/CyclinE, IC50: 0.7 μM

CDK2/CyclinA, IC50: 0.7 μM

++

CDK5/p35, IC50: 0.16 μM

99%+
Narazaciclib ++++

CDK4/CyclinD1, IC50: 3.87 nM

++++

CDK6/CyclinD1, IC50: 9.82 nM

RET 99%+
Palbociclib ++++

CDK4/CyclinD1, IC50: 11 nM

CDK4/CyclinD3, IC50: 9 nM

+++

CDK6/CyclinD2, IC50: 15 nM

99%
Abemaciclib ++++

CDK4, IC50: 2 nM

++++

CDK6, IC50: 10 nM

99%
Ribociclib ++++

CDK4, IC50: 10 nM

+++

CDK6, IC50: 39 nM

98%
Palbociclib isethionate ++++

CDK4/CyclinD1, IC50: 11 nM

CDK4/CyclinD3, IC50: 9 nM

+++

CDK6/CyclinD2, IC50: 15 nM

99%+
BS-181 HCl +++

CDK7, IC50: 21 nM

99%+
(E/Z)-THZ1 2HCl ++++

CDK7, IC50: 3.2 nM

99%+
LDC4297 ++++

CDK7, IC50: 0.13 nM

99%+
Senexin A +

CDK19, Kd: 0.31 μM

+

CDK8, Kd: 0.83 μM

99%
MSC2530818 ++++

CDK8, IC50: 2.6 nM

99%+
Wogonin 99%+
Riviciclib HCl ++

CDK1/CyclinB, IC50: 79 nM

+

CDK2/CyclinE, IC50: 2.54 μM

CDK2/CyclinA, IC50: 224 nM

++

CDK4/CyclinD1, IC50: 63 nM

+

CDK6/CyclinD3, IC50: 396 nM

+

CDK7/CyclinH, IC50: 2.87 μM

+++

CDK9/CyclinT1, IC50: 20 nM

98%
LDC000067 +

CDK2, IC50: 2.441 μM

++

CDK9, IC50: 44 nM

98%
Flavopiridol +++

CDK1, IC50: 40 nM

+++

CDK2, IC50: 40 nM

+++

CDK4, IC50: 40 nM

+++

CDK6, IC50: 40 nM

+

CDK7, IC50: 300 nM

+++

CDK9, IC50: 20 nM

99%+
LY2857785 +

CDK7, IC50: 0.246 μM

+++

CDK8, IC50: 0.016 μM

+++

CDK9, IC50: 0.011 μM

99%+
AZD-5438 +++

CDK1, IC50: 16 nM

++++

CDK2, IC50: 6 nM

+++

CDK9, IC50: 20 nM

99%+
ML167 ++

CLK4, IC50: 136 nM

Dyrk1B , IC50: 1648 nM

99%+
(E/Z)-TG003 +++

mCLK4, IC50: 15 nM

mCLK1, IC50: 200 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Flavopiridol HCl 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].

Flavopiridol HCl 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
A2780/TAX-R human ovarian carcinoma cell Proliferation assay Inhibition of A2780/TAX-R human ovarian carcinoma cell proliferation, IC50=78 nM 12190313

Flavopiridol HCl 动物研究

Dose Mice: 5 mg/kg, 7.5 mg/kg[3] (i.p.) Rat: 0.01 mg/kg- 5 mg/kg[4] (i.p.)
Administration i.p.

Flavopiridol HCl 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 <<

Flavopiridol HCl 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.

Flavopiridol HCl 实验方案

计算器
存储液制备 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

Flavopiridol HCl 技术信息

CAS号131740-09-5
分子式C21H21Cl2NO5
分子量 438.3
SMILES Code O=C1C=C(C2=CC=CC=C2Cl)OC3=C1C(O)=CC(O)=C3[C@@H]4[C@H](O)CN(C)CC4.[H]Cl
MDL No. MFCD26792554
别名 HMR-1275 Hydrochloride; L86-8275 Hydrochloride; L-868,275; HL 275; Flavopiridol (hydrochloride); DSP-2033; HMR-1275; Alvocidib; NSC 649890; Alvocidib Hydrochloride; Flavopiridol Hydrochloride
运输蓝冰
InChI Key LGMSNQNWOCSPIK-LWHGMNCYSA-N
Pubchem ID 9910986
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C

动物实验配方

PO 0.5% CMC-Na 50 mg/mL suspension

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