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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $61 | - | In Stock | |
| 5 mg | $147 | - | In Stock | |
| 10 mg | $222 | - | In Stock | |
| 25 mg | Preferential | - | In Stock | |
| 50 mg | Preferential | - | 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 | Del:5 nM, EGFR (WT):307 nM, ERG26 current (human):>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 | 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/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| 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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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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