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PHA-848125

CAS No. 802539-81-7

PHA-848125 ( Milciclib;PHA 848125 )

Catalog No. M16004 CAS No. 802539-81-7

A potent, selective, brain penetrant and orally available dual CDK and TRK inhibitor with IC50 of 45 and 53 nM for CDK2/cyclin A and TrkA, respectively; shows cross-reactivity with other CDKs (CDK1/4/5/7), TrkB/C, Kit, Abl and PDGFR (IC50s<1 uM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    PHA-848125
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective, brain penetrant and orally available dual CDK and TRK inhibitor with IC50 of 45 and 53 nM for CDK2/cyclin A and TrkA, respectively; shows cross-reactivity with other CDKs (CDK1/4/5/7), TrkB/C, Kit, Abl and PDGFR (IC50s<1 uM).
  • Description
    A potent, selective, brain penetrant and orally available dual CDK and TRK inhibitor with IC50 of 45 and 53 nM for CDK2/cyclin A and TrkA, respectively; shows cross-reactivity with other CDKs (CDK1/4/5/7), TrkB/C, Kit, Abl and PDGFR (IC50s<1 uM); nhibits cell proliferation of a wide panel of tumoral cell lines with submicromolar IC50; shows significant antitumor activity in various human xenografts.Brain Cancer Phase 2 Clinical
  • Synonyms
    Milciclib;PHA 848125
  • Pathway
    Angiogenesis
  • Target
    CDK
  • Recptor
    CDK2/CyclinA; CDK4/CyclinD1; CDK5/p35; CDK7/CyclinH; TrkA
  • Research Area
    Cancer
  • Indication
    Brain Cancer

Chemical Information

  • CAS Number
    802539-81-7
  • Formula Weight
    460.57
  • Molecular Formula
    C25H32N8O
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    O=C(C1=NN(C)C2=C1C(C)(C)CC3=CN=C(NC4=CC=C(N5CCN(C)CC5)C=C4)N=C23)NC
  • Chemical Name
    1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide, 4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Brasca MG, et al. J Med Chem. 2009 Aug 27;52(16):5152-63.
2. Degrassi A, et al. Mol Cancer Ther. 2010 Mar;9(3):673-81.
3. Albanese C, et al. Mol Cancer Ther. 2010 Aug;9(8):2243-54.
4. Albanese C, et al. Br J Pharmacol. 2013 May;169(1):156-66.
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