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PF-6274484

Name: PF-6274484
Brand: TargetMol
SKU: T22396
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T22396Cas No. 1035638-91-5

Alias PF 6274484

PF-6274484, a high affinity, irreversible covalent inhibitor of EGFR kinase with Ki of 0.14 nM, inhibits the autophosphorylation of wild-type EGFR in A549 cells and EGFRL858R/T790M in H1975 cells with IC50 of 5.8 nM and 6.6 nM, respectively.

PF-6274484

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Purity: 97.71%

Catalog No. T22396Alias PF 6274484Cas No. 1035638-91-5

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$34	In Stock	In Stock
5 mg	$55	In Stock	In Stock
10 mg	$93	In Stock	In Stock
25 mg	$197	In Stock	In Stock
50 mg	$369	In Stock	In Stock
100 mg	$549	In Stock	In Stock
500 mg	$1,190	-	In Stock
1 mL x 10 mM (in DMSO)	$61	In Stock	In Stock

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In Stock Estimated shipping dateUSA 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:97.71%

Appearance:Solid

Color:White

Resource Download

COA HPLC HNMR LCMS

Product Introduction

PF-6274484 AI Summary

PF-6274484 shows bioactivities related to the inhibition of PF-06422899 binding to EGFR in human A431 cells with a Ki of 0.14 nM and also inhibits PF-06422899 binding to recombinant C-terminal FLAG-tagged DUS2L expressed in HEK293T cells with an IC50 of 1600.0 nM. It exhibits selectivity towards specific EGFR mutations and demonstrates potent inhibition of EGFR autophosphorylation in response to different stimuli, with IC50 values in the low nanomolar range, indicating potential therapeutic relevance in targeting specific types of EGFR-driven cancers..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	PF-6274484, a high affinity, irreversible covalent inhibitor of EGFR kinase with Ki of 0.14 nM, inhibits the autophosphorylation of wild-type EGFR in A549 cells and EGFRL858R/T790M in H1975 cells with IC50 of 5.8 nM and 6.6 nM, respectively.
Targets&IC50	EGFR (WT):0.18 nM (Ki), EGFR:0.14 nM(Ki)
Synonyms	PF 6274484

Chemical Properties

Molecular Weight	372.78
Formula	C₁₈H₁₄ClFN₄O₂
Cas No.	1035638-91-5
Smiles	COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)C=C
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 65 mg/mL (174.37 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6825 mL	13.4127 mL	26.8255 mL	134.1274 mL
5 mM	0.5365 mL	2.6825 mL	5.3651 mL	26.8255 mL
10 mM	0.2683 mL	1.3413 mL	2.6825 mL	13.4127 mL
20 mM	0.1341 mL	0.6706 mL	1.3413 mL	6.7064 mL
50 mM	0.0537 mL	0.2683 mL	0.5365 mL	2.6825 mL
100 mM	0.0268 mL	0.1341 mL	0.2683 mL	1.3413 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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent 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 TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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