Free shipping on all orders over $ 500

Flavopiridol hydrochloride

Cat. No. M3483

Flavopiridol hydrochloride Structure

Synonym: NSC 649890 HCl

Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 280 In stock
100mg USD 440 In stock
200mg USD 650 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Flavopiridol hydrochloride is a potent cyclin-dependent kinases inhibitor with an IC50 of 100 nM. Preclinically, flavopiridol is the first cyclin-dependent kinase inhibitor. At the nanomolar concentrations, flavoporidol hydrochloride prevented rhabdoid cell growth with an IC50 ranging from 50 to 200 nM. Meanwhile, flavopiridol hydrochloride induced G1 and G2 arrest and apoptosis in vitro in a concentration-dependent manner. These influences were associated with the down- regulation of cyclin D1, up- modulation of p21, and induction of caspase 3/7 activities. At a dose of 7.5 mg/kg, flavopiridol markedly suppress the growth of xenografted rhabdoid tumors. That was associated with the induction of p21 and downregulation of cyclin D1. Treatment of flavopiridol decreased the activities of CDK2 and potently prevented cell proliferation with an IC50 ranging from 43 to 83 nM in HNSCC cells.

Protocol
Cell Experiment
Cell lines SUDHL4, SUDHL6, Jurkat, MOLT4, and HL60
Preparation method Growing cells at a density of 1 × 106 cells/mL are exposed to Flavopiridol for different concentrations and time periods. DNA is extracted. Briefly, washing cells once with cold phosphate-buffered saline (PBS) and lysing with 3 mL lysis buffer (5 mM Tris-HCL [pH 7.5]; 20 mM EDTA; 0.5% Triton X-100) for 15 minutes at 4 °C. The chromatin of the cell lysates is isolated by centrifugation (20 minutes at 26,000g, 4 °C). The supernatants containing small DNA fragments are extracted sequentially with phenol, phenol:chloroform (1:1), and chloroform. Nucleic acids are precipitated in 0.5 M NaCl, 90% ethanol at -20 °C overnight. Then digested RNA by bovine RNAaseA (60 μg/mL). After sequential reextraction and reprecipitation, DNA is dissolved in 10 mM Tris-HCL (pH 7.5), 1 mM EDTA, 0.5% sodium dodecyl sulfate (SDS) before electrophoresis on 1.6% agarose gel.
Concentrations 0, 100 500, 5000 nM
Incubation time 14 hours
Animal Experiment
Animal models Human prostate cancer xenografts, PRXFI337 and PRXFI369, grown s.c. in nude mice [4] Human promyelocytic leukemia HL-60, human B-cell follicular lymphoma SUDHL-4, and acquired immunodeficiency syndrome (AIDS)-r
Formulation Water [4]; 1% DMSO [6]
Dosages 10 mg/kg/d [4]; 7.5 mg/kg/d [6]
Administration p.o.[4]; i.p. or i.v. [6]
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 438.3
Formula C21H20ClNO5.HCl
CAS Number 131740-09-5
Purity >99%
Solubility DMSO 80 mg/mL
Storage at -20°C
Related CDK Products
NU2058

NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and 26 μM for CDK2 and CDK1.

LDC000067

LDC000067 is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7.

RO-3306

RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases.

LDC4297

LDC4297 is a novel CDK7 inhibitor (IC50=0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs).

THZ1

THZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Flavopiridol hydrochloride, NSC 649890 HCl supplier, CDK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.