Mavelertinib


Catalog No. Size PriceQuantity
M32986-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

Mavelertinib is a selective, orally available 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).

Product information

CAS Number: 1776112-90-3

Molecular Weight: 415.42

Formula: C18H22FN9O2

Chemical 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]prop-2-enamide

Smiles: CN1C=C(NC2=NC(=NC3=C2N=CN3C)N2C[C@@H](NC(=O)C=C)[C@H](F)C2)C(=N1)OC

InChiKey: JYIUNVOCEFIUIU-GHMZBOCLSA-N

InChi: InChI=1S/C18H22FN9O2/c1-5-13(29)21-11-8-28(6-10(11)19)18-23-15(14-16(24-18)26(2)9-20-14)22-12-7-27(3)25-17(12)30-4/h5,7,9-11H,1,6,8H2,2-4H3,(H,21,29)(H,22,23,24)/t10-,11-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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

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). 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).

Products are for research use only. Not for human use.

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