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Flavopiridol/夫拉平度 {[allProObj[0].p_purity_real_show]}

货号：A172904 同义名： L86-8275; Alvocidib

Flavopiridol (Alvocidib)是一种广谱竞争性CDK抑制剂，靶向CDK1、CDK2和CDK4，IC50值分别为30 nM、170 nM和100 nM。

Flavopiridol/夫拉平度 化学结构 CAS号：146426-40-6
Flavopiridol/夫拉平度 化学结构
CAS号：146426-40-6
Flavopiridol/夫拉平度 3D分子结构
CAS号：146426-40-6
Flavopiridol/夫拉平度 化学结构 CAS号：146426-40-6
Flavopiridol/夫拉平度 3D分子结构 CAS号：146426-40-6
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Flavopiridol/夫拉平度 纯度/质量文件 产品仅供科研

货号：A172904 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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• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
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更多 >
产品名称 Autophagy ↓ 其他靶点 纯度
SBI-0206965 +++

ULK2, IC50: 711 nM

ULK1, IC50: 108 nM

 		95%
Hydroxychloroquine sulfate ✔ 99%
Valproic acid sodium ✔ HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

 		99%+
MRT68921 HCl ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

 		99%+
ROC-325 ✔ 99%+
Autophinib +++

Autophagy, IC50: 40 nM

 		99%
Lys05 ✔ 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。
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(C118L), Kd: 18.6 nM

CDK2(A144C), Kd: 9.7 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/CyclinD3, IC50: 9 nM

CDK4/CyclinD1, IC50: 11 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/CyclinD3, IC50: 9 nM

CDK4/CyclinD1, IC50: 11 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 +++

mCLK1, IC50: 200 nM

mCLK4, IC50: 15 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/夫拉平度 生物活性

靶点

  • CDK4

    CDK4, IC50:20-40 nM

  • CDK2

    CDK2, IC50:40 nM

  • CDK6

    CDK6, IC50:60 nM

  • CDK9

    CDK9, IC50:20 nM
描述 Flavopiridol is a pan CDK inhibitor with IC50 value of 30nM, 40nM, 20-40nM, 60nM, 875nM and 20nM for CDK1, 2, 4, 6, 7, 9 (measured by in vitro kinase assays), respectively[1][2].

It can inhibit the whole cell cycle progression through a variety of mechanisms related to CDK inactivation including:

1. Inhibition of CDK4/6 with cyclin D leads to decreased level of pRb-p107 and p130, as well as inactivation of E2F and stop in G1 progression;

2. Inhibition of cdk2 accompanied with cyclin A or E leads to further decreased phosphorylation and inactivation of Rb, as well as inactivation of E2F, and results in retardation in cell cycle progression through the S-phase and accumulation in G1 and G2;

3. Inhibition of CDK1 accompanied with cyclin A or B leads to inhibition of activation of topoisomerase activators, of lamin proteoglycans histone 1 protein and chromatin condensation, as well as results in retardation in cell cycle progression through S-phase and accumulation in G2 phase;

4. Inhibition of cdk7 accompanied with cyclin H complexes leads to reduced activation of cdk’s, such as CDK4 with cyclin D or CDK1 with cyclin B, and reduced activation of RNA polymerase;

5. Flavopiridol may directly influence expression of cyclin D1 and D3 or participate directly in the control of transcription and activation of RNA-polymerase.

Flavopiridol is able to induce apoptosis of tumor cells, including leukemia cells, head and neck tumors, breast carcinomas and non-small cell lung carcinoma cell lines, as well as normal cells in vitro after 6–48h with concentration ranging in 0.1–0.4uM[3].

Intraperitoneal treatment of 5mg/kg flavopiridol for 12 days showed antitumor activity in subcutaneous HN12 xenograft mice[4].

Clinical studies of flavopiridol of treatement for advanced solid tumors, ALL, AML, CLL, CML, mantle cell lymphoma, multiple myeloma, non-Hodgkin and other lymphomas, advanced sarcomas, breast, esophageal, head and neck, kidney, ovarian, pancreatic, gastric carcinomas and NSCLC are undergoing[5].
作用机制 Flavopiridol is an ATP-competitive inhibitor[6].

Flavopiridol/夫拉平度 细胞实验

Cell Line
Concentration Treated Time Description References
U2OS cells 2 μM 90-120 min To investigate the effect of Flavopiridol on transcription elongation inhibition, results showed a dramatic increase in fluorescence recovery of RPB1, while FRAP kinetics of TAF5 and TFIIB were unaffected. EMBO J. 2017 Sep 15;36(18):2710-2725.
human chondrocytes 250nM 5 h suppress IL-1β-induced inflammatory gene expression Osteoarthritis Cartilage. 2021 Jan;29(1):68-77.
bovine cartilage explants 60nM 6 days prevent IL-1β-induced cartilage degradation Osteoarthritis Cartilage. 2021 Jan;29(1):68-77.
HeLa cells 1 μM 30 min Flavopiridol effectively inhibited KPNB1 transcription past the poly(A) site Nat Struct Mol Biol. 2015 May;22(5):396-403.
LNCaP-abl cells 300 nM 1 h Flavopiridol inhibits CDK9 phosphorylation of RNA Pol II, blocking the transition of PIC to the elongation phase of transcription. PAF1 was trapped at the promoter after 1 h FP treatment and gradually traveled through the gene body upon release. Nat Commun. 2021 Nov 3;12(1):6318.
A549 cells 20 μM 24 h To evaluate the effect of Flavopiridol on the proliferation, apoptosis, clone formation, migration, and invasion ability of A549 cells. The results showed that Flavopiridol significantly inhibited the proliferation, clone formation, migration, and invasion ability of A549 cells and induced apoptosis. Signal Transduct Target Ther. 2020 May 22;5(1):54.
PDX282 0.1 µM 24 h To evaluate the inhibitory effect of Flavopiridol on PDX282 cells, results showed that Flavopiridol significantly inhibited cell proliferation and induced apoptosis. Hepatology. 2024 Jul 1;80(1):55-68.
PDX303 0.1 µM 24 h To evaluate the inhibitory effect of Flavopiridol on PDX303 cells, results showed that Flavopiridol significantly inhibited cell proliferation and induced apoptosis. Hepatology. 2024 Jul 1;80(1):55-68.
PDX214 0.1 µM 24 h To evaluate the inhibitory effect of Flavopiridol on PDX214 cells, results showed that Flavopiridol had less effect on PDX214 cells in terms of cell viability. Hepatology. 2024 Jul 1;80(1):55-68.

Flavopiridol/夫拉平度 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Lung cancer xenograft model Intraperitoneal injection 8 mg/kg Three times per week for 41 days To evaluate the effect of Flavopiridol on tumor growth in the lung cancer xenograft model. The results showed that Flavopiridol significantly inhibited tumor growth, reducing tumor volume and weight. Signal Transduct Target Ther. 2020 May 22;5(1):54.
Mice ACL rupture model Intraperitoneal injection 2.5mg/kg 3 times per week for 4 weeks Reduce inflammation and osteoarthritis progression after ACL rupture Osteoarthritis Cartilage. 2021 Jan;29(1):68-77.
Mice PDX282 tumor model Intraperitoneal injection 5 mg/kg 3 times per week for 11 days To evaluate the therapeutic effect of Flavopiridol on the PDX282 tumor model, results showed that Flavopiridol significantly reduced tumor volume but also caused weight loss and unexpected death. Hepatology. 2024 Jul 1;80(1):55-68.

Flavopiridol/夫拉平度 动物研究

Dose Mice: min = 5 mg/kg, max = 7.5 mg/kg[6]
Administration i.p.
Pharmacokinetics
Animal Mice
AUC0→∞ 1.6 h (i.p.)

Flavopiridol/夫拉平度 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
NCT03604783 Advanced Solid Tumors Phase 1 Not yet recruiting May 2021 United States, Wisconsin ... 展开 >> Medical College of Wisconsin Not yet recruiting Milwaukee, Wisconsin, United States, 53226 Contact: Katy C Schroeder, BSN, RN, OCN    414-805-8843       Principal Investigator: Ben George, MD 收起 <<
NCT00055380 Cancer Phase 1 Completed - United States, Maryland ... 展开 >> National Institute of Dental And Craniofacial Research (NIDCR) Bethesda, Maryland, United States, 20892 收起 <<
NCT00003004 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 <<

Flavopiridol/夫拉平度 参考文献

[1]Montagnoli A, Valsasina B, et al. A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat Chem Biol. 2008 Jun;4(6):357-65.

[2]Aleem E, Arceci RJ, et al. Targeting cell cycle regulators in hematologic malignancies. Front Cell Dev Biol. 2015 Apr 9;3:16.

[3]Sedlacek HH, et al. Mechanisms of action of flavopiridol. Crit Rev Oncol Hematol. 2001 May;38(2):139-70.

[4]Roskoski R Jr, et al. Cyclin-dependent protein kinase inhibitors including palbociclib as anticancer drugs. Pharmacol Res. 2016 May;107:249-275.

[5]Li Y, Zhang J, et al. Insights on Structural Characteristics and Ligand Binding Mechanisms of CDK2. Int J Mol Sci. 2015 Apr 24;16(5):9314-40.

Flavopiridol/夫拉平度 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.49mL

0.50mL

0.25mL

12.44mL

2.49mL

1.24mL

24.89mL

4.98mL

2.49mL

Flavopiridol/夫拉平度 技术信息

CAS号146426-40-6
分子式C21H20ClNO5
分子量 401.84
SMILES Code O=C1C=C(C2=CC=CC=C2Cl)OC3=C1C(O)=CC(O)=C3[C@@H]4[C@H](O)CN(C)CC4
MDL No. MFCD20501884
别名 L86-8275; Alvocidib; HL 275; NSC 649890; HMR-1275
运输蓝冰
InChI Key BIIVYFLTOXDAOV-YVEFUNNKSA-N
Pubchem ID 5287969
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C
溶解方案

DMSO: 35 mg/mL(87.1 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

Tags: Flavopiridol | 146426-40-6 | HMR-1275 | Alvocidib | L86-8275 | HMR1275 | HMR 1275 | CDK Inhibitor | Cell Cycle/DNA Damage | Autophagy | Anti-infection | Apoptosis | CDK | Autophagy | HIV | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Flavopiridol/夫拉平度 纯度/质量文件 | Flavopiridol/夫拉平度 亚型比较 | Flavopiridol/夫拉平度 生物活性 | Flavopiridol/夫拉平度 动物研究 | Flavopiridol/夫拉平度 临床数据 | Flavopiridol/夫拉平度 参考文献 | Flavopiridol/夫拉平度 实验方案 | Flavopiridol/夫拉平度 技术信息

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