Flavopiridol HCl (Alvocidib)

SKU: orb1305264

Description

Flavopiridol hydrochloride

Research Area

Cell Biology

Key Properties

• CAS Number: 131740-09-5
• MW: 438.30
• Purity: >98%
• Formula: C₂₁H₂₀ClNO₅ HCl
• SMILES: Cl.CN1CC[C@@H]([C@H](O)C1)c1c(O)cc(O)c2c1oc(cc2=O)-c1ccccc1Cl
• Target: Kinase
• Solubility: Soluble in DMSO (up to 40 mg/ml) or in Water (up to 40 mg/ml).

Bioactivity

• Target IC50:
  PKC:14000 nM|CDK1:40 nM|MAP:19000 nM|CDK6:40 nM|EGFR:22000 nM|CDK4:40 nM|CDK2:40 nM|CDK7:300 nM
• In Vivo:
  Flavopiridol induces G1 phase arrest and inhibits CDK2 and CDK4 in human breast cancer cells in a time- and concentration-dependent manner. A short-term treatment of approximately 12 hours with Flavopiridol triggers apoptosis in hematopoietic cell lines, including SUDHL4, SUDHL6 (B-cell lines), Jurkat, MOLT4 (T-cell lines), and HL60 (myeloid). Additionally, Flavopiridol treatment induces significant AKT-Ser473 phosphorylation in the human glioblastoma T98G cell line. In clonogenic assays, Flavopiridol demonstrates potent cytotoxicity across 23 human tumor models, with an average IC70 of 8 ng/mL.
• In Vitro:
  Intravenous administration of 7.5 mg/kg Flavopiridol in mice with the SUDHL-4 subcutaneously injected lymphoma model resulted in significant tumor reduction, with the majority (3/4) or complete disappearance (1/2) of tumors. Notably, two animals remained symptom-free for over 60 days, achieving an overall tumor growth delay of 73.2%. When administered orally at the maximum tolerable dose of 10 mg/kg Flavopiridol daily during days 1-4 and 7-11, the treatment contributed to tumor regression in PRXF1337 and sustained tumor stasis for four weeks in PRXF1369. Furthermore, continuous intravenous or intraperitoneal injection of 7.5 mg/kg Flavopiridol over five days led to complete tumor regression in 11 out of 12 late-stage subcutaneous (sc) human HL-60 xenografted mice, with the treated mice remaining disease-free for several months post-treatment.
• Cell Research:
  Cells grown at a density of 1 × 106 cells/mL are exposed to Flavopiridol for different concentrations and time periods. DNA is extracted. Briefly, cells are washed once with cold phosphate-buffered saline (PBS) and lysed 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 26,000 g, 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. RNA is then digested 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. (Only for Reference)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

L 86-8275; Alvocidib; NSC-649890

Compound Identifiers

PubChem CID

9910986