1. Cell Cycle/DNA Damage
    Autophagy
  2. CDK
    Autophagy

Flavopiridol (Synonyms: L868275; HMR-1275; Alvocidib)

Cat. No.: HY-10005 Purity: 99.11%
Handling Instructions

Flavopiridol is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of around 40 nM.

For research use only. We do not sell to patients.
Flavopiridol Chemical Structure

Flavopiridol Chemical Structure

CAS No. : 146426-40-6

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
5 mg $50 In-stock
10 mg $70 In-stock
50 mg $310 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Flavopiridol is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of around 40 nM.

IC50 & Target

IC50: 40 nM (CDK)

In Vitro

Flavopiridol (2 μM) robustly induces a distinct pattern of ER stress in CLL cells that contributes to cell death through IRE1-mediated activation of ASK1 and possibly downstream caspases[1]. Flavopiridol results in potent upregulation of a number of PRGs in treatments lasting 4-24 h. Flavopiridol has and immediate and long-term effect on the expression of several PRGs. In serum starved cells re-stimulated with serum, flavopiridol also inhibits the expression of these genes, but subsequently, JUNB, GADD45B and EGR1 are upregulated in the presence of flavopiridol[2].

Clinical Trial
Sponsor Condition Start Date Phase
Sidney Kimmel Comprehensive Cancer Center Acute myelogenous leukemia 2011-05-31 Phase 2
Sidney Kimmel Comprehensive Cancer Center Acute myelogenous leukemia 2011-04-30 Phase 2
Testis tumor 2013-05-31 Phase 2
Ovary tumor 2013-05-31 Phase 2
Eastern Cooperative Oncology Group Acute myelogenous leukemia 2008-10-31 Phase 2
References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.4886 mL 12.4428 mL 24.8855 mL
5 mM 0.4977 mL 2.4886 mL 4.9771 mL
10 mM 0.2489 mL 1.2443 mL 2.4886 mL
Kinase Assay
[1]

Briefly, lysates containing approximately 3×106 cells are incubated with 50 μM LEVD-AFC (caspase 4 substrate) or LETD-AFC (caspase 8 substrate) containing 10 mM dithiothretiol (DTT). caspase 4 activity is measured one hour after addition of substrate and caspase 8 activity is measured 30 minutes after addition of substrate. Release of free AFC is measured with a Beckman-Coulter DTX 880 multimode detector.

Cell Assay
[1]

The cells treated with flavopiridol are washed after 4 hours with PBS and resuspended in regular growth medium (RPMI 1640) supplemented with 10% human serum and antibiotics for the remainder of the incubation time. In the case of flavopiridol/chloroquine samples, chloroquine is re-added in the fresh media after flavopiridol is washed at 4 hours. For all the other conditions, cells are incubated with the respective drugs for 24 hours continuously.

References
M.Wt

401.84

Formula

C₂₁H₂₀ClNO₅

CAS No.

146426-40-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

Purity: 99.11%

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Product Name:
Flavopiridol
Cat. No.:
HY-10005
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