store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 198.00 | |
10 mg | In stock | $ 319.00 | |
25 mg | In stock | $ 542.00 | |
50 mg | In stock | Inquiry | |
1 mL * 10 mM (in DMSO) | In stock | $ 226.00 |
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 | Del:5 nM, EGFR (WT):307 nM, hERG26 current:>100 μM, T790M/Del:3 nM, T790M/L858R:12 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]. |
Synonyms | PF 06747775, PFE-X775, PF-06747775, PF-7775, PF 6747775, PF6747775 |
Molecular Weight | 415.42 |
Formula | C18H22FN9O2 |
CAS No. | 1776112-90-3 |
store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (72.22 mM), Sonication is recommended.
H2O: <0.1 mg/mL
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Mavelertinib 1776112-90-3 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR PF 06747775 PFE-X775 PF-06747775 PF-7775 PF 6747775 PF06747775 PF6747775 PF-6747775 inhibitor inhibit