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Mavelertinib

🥰Excellent
Catalog No. T21322Cas No. 1776112-90-3
Alias PFE-X775, PF-7775, PF6747775, PF-06747775, PF 6747775, PF 06747775

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.

Mavelertinib

Mavelertinib

🥰Excellent
Purity: 100%
Catalog No. T21322Alias PFE-X775, PF-7775, PF6747775, PF-06747775, PF 6747775, PF 06747775Cas No. 1776112-90-3
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 SizePriceAvailabilityQuantity
1 mg$61In Stock
5 mg$147In Stock
10 mg$222In Stock
25 mgInquiryIn Stock
50 mgInquiryIn Stock
1 mL x 10 mM (in DMSO)$226In Stock
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Purity:100%
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Product Introduction

Bioactivity
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].
AliasPFE-X775, PF-7775, PF6747775, PF-06747775, PF 6747775, PF 06747775
Chemical Properties
Molecular Weight415.42
FormulaC18H22FN9O2
Cas No.1776112-90-3
SmilesCOc1nn(C)cc1Nc1nc(nc2n(C)cnc12)N1C[C@@H](F)[C@@H](C1)NC(=O)C=C
Relative Density.1.52 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM2.4072 mL12.0360 mL24.0720 mL120.3601 mL
5 mM0.4814 mL2.4072 mL4.8144 mL24.0720 mL
10 mM0.2407 mL1.2036 mL2.4072 mL12.0360 mL
20 mM0.1204 mL0.6018 mL1.2036 mL6.0180 mL
50 mM0.0481 mL0.2407 mL0.4814 mL2.4072 mL

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