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Mavelertinib (PF-06747775) is an orally available, selective and potent EGFR tyrosine kinase (EGFR TKI) inhibitor with inhibitory effects on T790M/L858R and T790M/Del, and can be used in the study of oncology and respiratory diseases.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $61 | In Stock | |
5 mg | $147 | In Stock | |
10 mg | $222 | In Stock | |
25 mg | Inquiry | In Stock | |
50 mg | Inquiry | In Stock | |
1 mL x 10 mM (in DMSO) | $226 | In Stock |
Description | Mavelertinib (PF-06747775) is an orally available, selective and potent EGFR tyrosine kinase (EGFR TKI) inhibitor with inhibitory effects on T790M/L858R and T790M/Del, and can be used in the study of oncology and respiratory diseases. |
Targets&IC50 | EGFR (WT):307 nM, T790M/L858R:12 nM, T790M/Del:3 nM, hERG26 current:>100 μM, Del:5 nM, L858R:4 nM |
In vitro | Inhibiting the hERG26 current with an IC50 greater than 100 μM, Mavelertinib exhibits selectivity over wild-type EGFR (IC50=307 nM)[1]. With less than 50% effect or inhibition against all nonkinase targets at 10 μM, Mavelertinib demonstrates its selectivity[1]. |
In vivo | Following oral administration (1 mg/kg to mouse, rat, and dog), Mavelertinib exhibits low to moderate oral bioavailability (mouse 60%, rat 11%, dog 66%)[1]. 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), Mavelertinib exhibits short plasma half-lives (mouse 0.56, rat 0.28, dog 1.3 h) following intravenous administration[1]. |
Alias | PFE-X775, PF-7775, PF6747775, PF-06747775, PF 6747775, PF 06747775 |
Molecular Weight | 415.42 |
Formula | C18H22FN9O2 |
Cas No. | 1776112-90-3 |
Smiles | COc1nn(C)cc1Nc1nc(nc2n(C)cnc12)N1C[C@@H](F)[C@@H](C1)NC(=O)C=C |
Relative Density. | 1.52 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (72.22 mM), Sonication is recommended. H2O: <0.1 mg/mL | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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