1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. Mavelertinib

Mavelertinib (Synonyms: PF-06747775)

Cat. No.: HY-12972 Purity: >99.0%
Handling Instructions

Mavelertinib is a selective, orally active and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).

For research use only. We do not sell to patients.

Mavelertinib Chemical Structure

Mavelertinib Chemical Structure

CAS No. : 1776112-90-3

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Estimated Time of Arrival: December 31
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Description

Mavelertinib is a selective, orally active and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC)[1][2][3].

IC50 & Target

IC50: 3 nM (T790M/Del), 4 nM (L858R), 5 nM (Del), 12 nM (T790M/L858R), 307 nM (wild-type)[1]

In Vitro

Mavelertinib exhibits selectivity over wild-type EGFR (IC50=307 nM)[1].
Mavelertinib (10 μM) exhibits less than 50% effect or inhibition against all nonkinase targets[1].
Mavelertinib inhibits the hERG26 current with an IC50 > 100 μM[1].

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).
Molecular Weight

415.42

Formula

C₁₈H₂₂FN₉O₂

CAS No.

1776112-90-3

SMILES

C=CC(N[[email protected]@H]1CN(C2=NC(NC3=CN(C)N=C3OC)=C4N=CN(C)C4=N2)C[[email protected]]1F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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Keywords:

MavelertinibPF-06747775PF06747775PF 06747775EGFREpidermal growth factor receptorErbB-1HER1tyrosinekinaseTKIDelL858RdoublemutantsT790M/L858RT790M/Delnon-small-cell lungcancerNSCLCInhibitorinhibitorinhibit

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Mavelertinib
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