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ChemicalBook >  Product Catalog >  Biochemical Engineering >  Biochemical Reagents >  Agonist Inhibitors >  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

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

Basic information Safety Supplier Related

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 Basic information

Product 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
Synonyms:
  • MAVELERTINIB
  • 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
  • PF-06747775
  • CPI-637
  • N-[(3R,4R)-4-fluoro-1-[6-[(3-methoxy-1-methylpyrazol-4-yl)amino]-9-methylpurin-2-yl]pyrrolidin-3-yl]prop-2-enamide
  • PF 6747775
  • 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]-
  • Mavelertinib( PF-06747775)
CAS:
1776112-90-3
MF:
C18H22FN9O2
MW:
415.42
Mol File:
1776112-90-3.mol
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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 Chemical Properties

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
InChIKey
JYIUNVOCEFIUIU-GHMZBOCLSA-N
SMILES
CN1C2=NC(N3C[C@@H](NC(C=C)=O)[C@H](F)C3)=NC(NC(C(OC)=N4)=CN4C)=C2N=C1
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Safety Information

WGK Germany 
WGK 3
Storage Class
11 - Combustible Solids
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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 Usage And Synthesis

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 available, potent 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).

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)acrylamideSupplier

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