| Identification | Back Directory | [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 | [CAS]
1428774-45-1 | [Synonyms]
EOS-61635
PF-06459988
PF-06459988 >=98% (HPLC)
1-((3R,4R)-3-(((5-chloro-1H-pyrazol-4-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)methyl)-4-methoxypyrrolidin-1-yl)prop-2-en-1-one
irreversible,oral,T790M,Inhibitor,EGFR,PF 06459988,PF-06459988,HER1,NSCLC,inhibit,PF06459988,Epidermal growth factor receptor,cancer,ErbB-1
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
2-Propen-1-one, 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-methoxy-1-pyrrolidinyl]- | [Molecular Formula]
C19H22ClN7O3 | [MDL Number]
MFCD28987462 | [MOL File]
1428774-45-1.mol | [Molecular Weight]
431.88 |
| Chemical Properties | Back Directory | [density ]
1.50±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 50 mg/mL (115.77 mM) | [form ]
Solid | [pka]
11.26±0.50(Predicted) | [color ]
White to off-white | [InChIKey]
ODMXWZROLKITMS-RISCZKNCSA-N | [SMILES]
ClC1=CNC2=C1C(OC[C@@H]3[C@@H](OC)CN(C(C=C([H])[H])=O)C3)=NC(NC4=CN(C)N=C4)=N2 |
| Hazard Information | Back Directory | [Uses]
PF-06459988 is an orally activity, irreversible and mutant-selective inhibitor of EGFR mutant forms. PF-06459988 demonstrates high potency and specificity to the T790M-containing double mutant EGFRs. PF-06459988 can be used for the research of cancer[1]. | [Biological Activity]
PF-06459988 is an orally available irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant (EGFRm) forms including the secondary acquired resistance mutation T790M. PF-06459988 has minimal activity against wild-type EGFR (WT EGFR). | [References]
[1] Cheng H, et al. Discovery of 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 (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. J Med Chem. 2016 Mar 10;59(5):2005-24. doi: 10.1021/acs.jmedchem.5b01633. Epub 2016 Jan 28. DOI:10.1021/acs.jmedchem.5b01633 |
|
|