| Identification | Back Directory | [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 | [CAS]
1776112-90-3 | [Synonyms]
CPI-637
PF 6747775
PF-06747775
MAVELERTINIB
Mavelertinib( PF-06747775)
N-[(3R,4R)-4-fluoro-1-[6-[(3-methoxy-1-methylpyrazol-4-yl)amino]-9-methylpurin-2-yl]pyrrolidin-3-yl]prop-2-enamide
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
2-Propenamide, N-[(3R,4R)-4-fluoro-1-[6-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]-9-methyl-9H-purin-2-yl]-3-pyrrolidinyl]- | [Molecular Formula]
C18H22FN9O2 | [MDL Number]
MFCD29079007 | [MOL File]
1776112-90-3.mol | [Molecular Weight]
415.42 |
| Chemical Properties | Back Directory | [density ]
1.52±0.1 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
DMSO: 20mg/mL, clear | [form ]
powder | [pka]
12.93±0.40(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
PF 06747775 is an orally available inhibitor of the epidermall growth factor receptor (EGFR) mutant form T790M showing antineoplastic activity. | [Biological Activity]
PF-06747775 is an orally availablepotent and selective inhibitor of the epidermal growth factor receptor) mutant form T790M (EGFR T790M inhibitor). PF-06747775 exhibits minimal activity against wild type EGFR. | [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)[1].
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)[1]. | Animal Model: | Female Nu/Nu mice[1] | | Dosage: | 1 mg/kg (Pharmacokinetic Analysis) | | Administration: | P.o. and i.v. administration | | Result: | Oral bioavailability (60%), T1/2 (1.48 h). |
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