PF-06747775

CAS No. 1776112-90-3

PF-06747775( PF 06747775 | PF06747775 | PF 6747775 )

Catalog No. M12674 CAS No. 1776112-90-3

A potent, selective, irreversible EGFR mutants with IC50 of 12, 3, 4 and 5 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    PF-06747775
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective, irreversible EGFR mutants with IC50 of 12, 3, 4 and 5 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively.
  • Description
    A potent, selective, irreversible EGFR mutants with IC50 of 12, 3, 4 and 5 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively; displays excellent selectivity over wild-type EGFR (IC50=307 nM), and desirable ADME properties, shows potential for treatment of EGFR T790M mutation in advanced NSCLC.Lung Cancer Phase 2 Clinical.
  • In Vitro
    Mavelertinib exhibits selectivity over wild-type EGFR (IC50=307 nM).Mavelertinib (10 μM) exhibits less than 50% e?ect or inhibition against all nonkinase targets.Mavelertinib inhibits the hERG26 current with an IC50 > 100 μM.
  • In Vivo
    Mavelertinib exhibits low to moderate oral bioavailability (mouse 60%, rat 11%, dog 66%) following oral administration (mouse 1, rat 30, dog 3 mg/kg).Mavelertinib exhibits short plasma half-lives (mouse 0.56, rat 0.28, dog 1.3 h) due to moderate to high plasma clearance (mouse 53, rat 49, dog 12 mL/min/kg) and low steady-state volume of distribution (mouse 1.48, rat 0.66, dog 0.94 L/kg) following intravenous administration (1 mg/kg to mouse, rat and dog). Animal Model:Female Nu/Nu mice Dosage:1 mg/kg (Pharmacokinetic Analysis) Administration:P.o. and i.v. administration Result:Oral bioavailability (60%), T1/2 (1.48 h).
  • Synonyms
    PF 06747775 | PF06747775 | PF 6747775
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR
  • Research Area
    Cancer
  • Indication
    Lung Cancer

Chemical Information

  • CAS Number
    1776112-90-3
  • Formula Weight
    415.433
  • Molecular Formula
    C18H22FN9O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 47.5 mg/mL (114.34 mM)
  • SMILES
    C=CC(N[C@@H]1CN(C2=NC(NC3=CN(C)N=C3OC)=C4N=CN(C)C4=N2)C[C@H]1F)=O
  • Chemical Name
    N-((3R,4R)-4-fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidin-3-yl)acrylamide

Shipping & Storage Information

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

Reference

1. Planken S, et al. J Med Chem. 2017 Apr 13;60(7):3002-3019. 2. Patel H, et al. Eur J Med Chem. 2017 May 11. pii: S0223-5234(17)30388-4. 3. Wang S, et al. J Hematol Oncol. 2016 Apr 12;9:34.
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