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HKI-357

Name: HKI-357
Brand: TargetMol
SKU: T11569
Price: 72 USD
Availability: InStock
Rating: 5 (10 reviews)

HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 (IC50s: 34 nM and 33 nM), effectively suppressing EGFR autophosphorylation (at Y1068), as well as AKT and MAPK phosphorylation.

Catalog No. T11569Cas No. 848133-17-5

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Purity:98.31%

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COA HNMR HPLC

HKI-357

Catalog No. T11569Cas No. 848133-17-5

HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 (IC50s: 34 nM and 33 nM), effectively suppressing EGFR autophosphorylation (at Y1068), as well as AKT and MAPK phosphorylation.

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.

Pack Size	Price	Availability
1 mg	$72	In Stock
5 mg	$155	In Stock
10 mg	$239	In Stock
25 mg	$487	In Stock
50 mg	$696	In Stock
100 mg	$987	In Stock
1 mL x 10 mM (in DMSO)	$197	In Stock

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Product Introduction

Bioactivity

Description	HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 (IC50s: 34 nM and 33 nM), effectively suppressing EGFR autophosphorylation (at Y1068), as well as AKT and MAPK phosphorylation.
Targets&IC50	ErbB2:33 nM, EGFR:34 nM
In vitro	HKI-357 also is effective in suppressing EGFR autophosphorylation (measured at residue Y1068), and AKT and MAPK phosphorylation in parental NCI-H1650 cells harboring the delE746-A750 EGFR mutation.HKI-357 (0.01-10 μM) is effective in suppressing ligand-induced EGFR autophosphorylation and its downstream signaling, as determined by AKT and MAPK phosphorylation in NCI-H1975 cells.

Chemical Properties

Molecular Weight	574.05
Formula	C₃₁H₂₉ClFN₅O₃
Cas No.	848133-17-5

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 30 mg/mL (52.2 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7420 mL	8.7100 mL	17.4201 mL	87.1004 mL
5 mM	0.3484 mL	1.7420 mL	3.4840 mL	17.4201 mL
10 mM	0.1742 mL	0.8710 mL	1.7420 mL	8.7100 mL
20 mM	0.0871 mL	0.4355 mL	0.8710 mL	4.3550 mL
50 mM	0.0348 mL	0.1742 mL	0.3484 mL	1.7420 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% 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 μLddH2O TargetMol | reagent

mix well and clarify

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

Dose Conversion

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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