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BLU-945

Name: BLU-945
Brand: TargetMol
SKU: T9754
Price: 32 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9754Cas No. 2660250-10-0

Alias BLU945, BLU 945

BLU-945 is a reversible, potent, highly selective, and orally available epidermal growth factor receptor tyrosine kinase inhibitor (TKIs). BLU-945 inhibits EGFR phosphorylation in EGFR L858R/T790M/C797S and EGFR ex19del/T790M/C797S mutant cell lines. BLU-945 can be used in lung cancer research, including non-small cell lung cancer (NSCLC).

BLU-945

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Purity: 99.16%

Catalog No. T9754Alias BLU945, BLU 945Cas No. 2660250-10-0

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$32	In Stock	In Stock
5 mg	$73	In Stock	In Stock
10 mg	$123	In Stock	In Stock
25 mg	$247	In Stock	In Stock
50 mg	$396	In Stock	In Stock
100 mg	$619	-	In Stock
200 mg	$877	-	In Stock
1 mL x 10 mM (in DMSO)	$268	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:99.16%

Appearance:Solid

Color:White to Yellow

Resource Download

COA HPLC HNMR

Product Introduction

Bioactivity

Description	BLU-945 is a reversible, potent, highly selective, and orally available epidermal growth factor receptor tyrosine kinase inhibitor (TKIs). BLU-945 inhibits EGFR phosphorylation in EGFR L858R/T790M/C797S and EGFR ex19del/T790M/C797S mutant cell lines. BLU-945 can be used in lung cancer research, including non-small cell lung cancer (NSCLC).
In vitro	BLU-945 exhibits subnanomolar activity against EGFR+/T790M and EGFR+/T790M/C797S mutants and maintains activity against EGFR activating mutations (L858R, ex19del), especially EGFR L858R; BLU-945 exhibits excellent inhibitory activity against the pEGFR H1975 cell line (IC50 = 1.1 nM), which is approximately 500-fold more potent than pEGFR A431 (EGFR-WT amplified cell line); in addition, BLU-945 can effectively inhibit EGFR phosphorylation in the Ba/F3 engineered cell line (L858R/T790M/C797S IC50 = 3.2 nM, ex19del/T790M/C797S IC50 = 4.0 nM)[1]；BLU-945 (1-10000μM) inhibits EGFR phosphorylation in EGFR L858R/T790M/C797S and EGFR ex19del/T790M/C797S mutant cell lines. [3]
In vivo	METHODS: BLU-945 (30, 100 mg/kg, twice daily) was administered to mice bearing NCI-H1975 xenografts. RESULTS BLU-945 at 100 mg/kg induced tumor stasis in mice bearing NCI-H1975 xenografts. [1]
Synonyms	BLU945, BLU 945

Chemical Properties

Molecular Weight	556.7
Formula	C₂₈H₃₇FN₆O₃S
Cas No.	2660250-10-0
Smiles	CO[C@@H]1CCN(C[C@@H]1F)c1nccc(Nc2cc3c(ccc(N4C[C@H](CS(C)(=O)=O)[C@H]4C)c3cn2)C(C)C)n1

Storage & Solubility Information

Storage

store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (449.07 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7963 mL	8.9815 mL	17.9630 mL	89.8150 mL
5 mM	0.3593 mL	1.7963 mL	3.5926 mL	17.9630 mL
10 mM	0.1796 mL	0.8981 mL	1.7963 mL	8.9815 mL
20 mM	0.0898 mL	0.4491 mL	0.8981 mL	4.4907 mL
50 mM	0.0359 mL	0.1796 mL	0.3593 mL	1.7963 mL
100 mM	0.0180 mL	0.0898 mL	0.1796 mL	0.8981 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