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Mavelertinib

Name: Mavelertinib
Brand: TargetMol
SKU: T21322
Price: 226 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰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

🥰Excellent

Purity: 99.89%

Catalog No. T21322Alias PFE-X775, PF-7775, PF6747775, PF-06747775, PF 6747775, PF 06747775Cas No. 1776112-90-3

Pack Size	Price	USA Warehouse	Global Warehouse
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

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Expected start date of shipmentUSA Warehouse [1-2 days] Global Warehouse [5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.89%

Resource Download

COA HNMR HPLC

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	T790M/Del:3 nM, EGFR (WT):307 nM, L858R:4 nM, Del:5 nM, T790M/L858R:12 nM, ERG26 current (human):＞100 μM
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

Chemical Properties

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 & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	2.4072 mL	12.0360 mL	24.0720 mL	120.3601 mL
5 mM	0.4814 mL	2.4072 mL	4.8144 mL	24.0720 mL
10 mM	0.2407 mL	1.2036 mL	2.4072 mL	12.0360 mL
20 mM	0.1204 mL	0.6018 mL	1.2036 mL	6.0180 mL
50 mM	0.0481 mL	0.2407 mL	0.4814 mL	2.4072 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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