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    PF-06459988
    PF-06459988

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V4473
    CAS #: 1428774-45-1Purity ≥98%

    Description: PF-06459988 is a novel, potent, orally bioavailable, third-generation, irreversible small molecule inhibitor of T790M-Containing EGFR Mutants with potential antineoplastic activity. First generation EGFR TKIs (gefitinib, erlotinib) provide significant clinical benefit for NSCLC cancer patients with oncogenic EGFR mutations. Ultimately, these patients' disease progresses, often driven by a second-site mutation in the EGFR kinase domain (T790M). Another liability of the first generation drugs is severe adverse events driven by inhibition of WT EGFR.  PF-06459988 was discovered as a novel, third generation irreversible inhibitor, which demonstrates (i) high potency and specificity to the T790M-containing double mutant EGFRs, (ii) minimal intrinsic chemical reactivity of the electrophilic warhead, (iii) greatly reduced proteome reactivity relative to earlier irreversible EGFR inhibitors, and (iv) minimal activity against WT EGFR.

    References:  2016 Mar 10;59(5):2005-24.


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    PF-06459988

    Name: PF-06459988
    CAS#: 1428774-45-1
    Chemical Formula: C19H22ClN7O3
    Exact Mass: 431.1473
    Molecular Weight: 431.881
    Elemental Analysis: C, 52.84; H, 5.13; Cl, 8.21; N, 22.70; O, 11.11
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: PF-6459988; PF 6459988; PF6459988; PF-06459988; PF06459988; PF 06459988;
    IUPAC/Chemical Name: 1-((3R,4R)-3-(((5-chloro-2-((1-methyl-1H-pyrazol-4-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)methyl)-4-methoxypyrrolidin-1-yl)prop-2-en-1-one
    InChi Key: ODMXWZROLKITMS-RISCZKNCSA-N
    InChi Code: InChI=1S/C19H22ClN7O3/c1-4-15(28)27-7-11(14(9-27)29-3)10-30-18-16-13(20)6-21-17(16)24-19(25-18)23-12-5-22-26(2)8-12/h4-6,8,11,14H,1,7,9-10H2,2-3H3,(H2,21,23,24,25)/t11-,14+/m1/s1
    SMILES Code: C=CC(N1C[[email protected]](COC2=C3C(NC=C3Cl)=NC(NC4=CN(C)N=C4)=N2)[[email protected]@H](OC)C1)=O


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