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PF-06747775

Chemical Structure : PF-06747775

CAS No.: 1776112-90-3

PF-06747775 (Mavelertinib;PF06747775)

Catalog No.: PC-60295Not For Human Use, Lab Use Only.

Mavelertinib (PF-06747775) is 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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Mavelertinib (PF-06747775) is 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.
PF-06747775 displays excellent selectivity over wild-type EGFR (IC50=307 nM), and desirable ADME properties.
PF-06747775 shows potential for treatment of EGFR T790M mutation in advanced NSCLC.

Physicochemical Properties

M.Wt 415.433
Formula C18H22FN9O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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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