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MEK&P38 MAPK

Flavopiridol (146426-40-6)

Flavopiridol competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2

Not Intended for Therapeutic Use. For research use only.

CAS: 146426-40-6 Category

Flavopiridol (146426-40-6) Description:

Alvocidib is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity. Check for active clinical trials or closed clinical trials using this agent.

Alvocidib is the free base form of a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity.

Flavopiridol (146426-40-6) Specifications:

Product Name Flavopiridol
Synonym L 86-8275; L-868275; L 868275; L868275; HMR 1274; HMR-1274; HMR1274; Flavopridol; Alvocidib;
Chemical Name 2-(2-chlorophenyl)-5,7-dihydroxy-8-((3R,4S)-3-hydroxy-1-methylpiperidin-4-yl)-4H-chromen-4-one
Drug Class N/A
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 146426-40-6
Molecular Formula C21H20ClNO5
Molecular Weight 401.84
Monoisotopic Mass
401.103 g/mol

 

MDL number MFCD00894265
InChIKey BIIVYFLTOXDAOV-PXAZEXFGSA-N
InChi Code InChI=1S/C21H20ClNO5/c1-23-7-6-12(17(27)10-23)19-14(24)8-15(25)20-16(26)9-18(28-21(19)20)11-4-2-3-5-13(11)22/h2-5,8-9,12,17,24-25,27H,6-7,10H2,1H3/t12-,17+/m1/s1
SMILES O=C1C=C(C2=CC=CC=C2Cl)OC3=C([[email protected]]4[[email protected]@H](O)CN(C)CC4)C(O)=CC(O)=C13
Form solid powder
Color Light yellow to yellow
Solubility  Soluble in DMSO
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application Flavopiridol is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.

 


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RIDADR NONH for all modes of transport

References:

  • 1: Zocchi L, Wu SC, Wu J, Hayama KL, Benavente CA. The cyclin-dependent kinase inhibitor flavopiridol (alvocidib) inhibits metastasis of human osteosarcoma cells. Oncotarget. 2018 May 4;9(34):23505-23518. doi: 10.18632/oncotarget.25239. eCollection 2018 May 4. PubMed PMID: 29805751; PubMed Central PMCID: PMC5955096.
  • 2: Bogenberger J, Whatcott C, Hansen N, Delman D, Shi CX, Kim W, Haws H, Soh K, Lee YS, Peterson P, Siddiqui-Jain A, Weitman S, Stewart K, Bearss D, Mesa R, Warner S, Tibes R. Combined venetoclax and alvocidib in acute myeloid leukemia. Oncotarget. 2017 Nov 3;8(63):107206-107222. doi: 10.18632/oncotarget.22284. eCollection 2017 Dec 5. PubMed PMID: 29291023; PubMed Central PMCID: PMC5739808.
  • 3: Zhou L, Zhang Y, Sampath D, Leverson J, Dai Y, Kmieciak M, Nguyen M, Orlowski RZ, Grant S. Flavopiridol enhances ABT-199 sensitivity in unfavourable-risk multiple myeloma cells in vitro and in vivo. Br J Cancer. 2018 Feb 6;118(3):388-397. doi: 10.1038/bjc.2017.432. Epub 2017 Dec 14. PubMed PMID: 29241222; PubMed Central PMCID: PMC5808038.
  • 4: Pawlak A, DE Miguel D, Kutkowska J, Obmińska-Mrukowicz B, Rapak A, Martinez-Lostao L. Flavopiridol Strongly Sensitizes Canine Lymphoma Cells to TRAIL-induced Apoptosis. Anticancer Res. 2017 Dec;37(12):6655-6665. PubMed PMID: 29187441.
  • 5: Lashgari A, Millau JF, Jacques PÉ, Gaudreau L. Global inhibition of transcription causes an increase in histone H2A.Z incorporation within gene bodies. Nucleic Acids Res. 2017 Dec 15;45(22):12715-12722. doi: 10.1093/nar/gkx879. PubMed PMID: 29036442; PubMed Central PMCID: PMC5727466.

1 review for Flavopiridol (146426-40-6)

  1. Cofttek

    Never had such good experience before,The Flavopiridol (146426-40-6) is high purity,also customer service is pretty nice !gotta try!!

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