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BMS-599626 Hydrochloride

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Catalog No. T5390Cas No. 873837-23-1
Alias AC480 Hydrochloride

BMS-599626 Hydrochloride (AC480 Hydrochloride) is an orally bioavailable inhibitor of the HER1, HER2, and HER4 tyrosine kinases (IC50 = 22, 32, and 190 nM, respectively) with potential antineoplastic activity, inhibiting the proliferation of tumor cells that overexpress these receptors.

BMS-599626 Hydrochloride

BMS-599626 Hydrochloride

😃Good
Purity: 99.98%
Catalog No. T5390Alias AC480 HydrochlorideCas No. 873837-23-1
BMS-599626 Hydrochloride (AC480 Hydrochloride) is an orally bioavailable inhibitor of the HER1, HER2, and HER4 tyrosine kinases (IC50 = 22, 32, and 190 nM, respectively) with potential antineoplastic activity, inhibiting the proliferation of tumor cells that overexpress these receptors.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$37-In Stock
5 mg$87-In Stock
10 mg$133-In Stock
25 mg$253-In Stock
50 mg$447-In Stock
100 mg$659-In Stock
1 mL x 10 mM (in DMSO)$109-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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Purity:99.98%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
BMS-599626 Hydrochloride (AC480 Hydrochloride) is an orally bioavailable inhibitor of the HER1, HER2, and HER4 tyrosine kinases (IC50 = 22, 32, and 190 nM, respectively) with potential antineoplastic activity, inhibiting the proliferation of tumor cells that overexpress these receptors.
Targets&IC50
HER1:22 nM, HER4:190 nM, HER2:32nM
In vitro
BMS-599626 Hydrochloride abrogates HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50s in the range of 0.24 to 1 μM.In GEO cells, HER1 phosphorylation is stimulated by treatment with EGF and is inhibited by BMS-599626 Hydrochloride (IC50=0. 75 μM).There is also nearly complete inhibition of EGF-dependent MAPK (0. 8 μM) but only partial inhibition of AKT signaling.The latter likely reflects the activation of AKT by multiple upstream signals.Treatment of N87 cells with BMS-599626 Hydrochloride leads to the inhibition of HER2 (0. 38 μM), which is expressed to a high level because of gene amplification, as well as MAPK and AKT phosphorylation (0.35 μM for both) [1].
In vivo
BMS-599626 Hydrochloride given before and during irradiation improved the radioresponse of HN5 tumors in vivo [2].
SynonymsAC480 Hydrochloride
Chemical Properties
Molecular Weight567.01
FormulaC27H28ClFN8O3
Cas No.873837-23-1
SmilesCl.Cc1c(NC(=O)OC[C@@H]2COCCN2)cn2ncnc(Nc3ccc4n(Cc5cccc(F)c5)ncc4c3)c12
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 90 mg/mL (158.73 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (5.82 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7636 mL8.8182 mL17.6364 mL88.1819 mL
5 mM0.3527 mL1.7636 mL3.5273 mL17.6364 mL
10 mM0.1764 mL0.8818 mL1.7636 mL8.8182 mL
20 mM0.0882 mL0.4409 mL0.8818 mL4.4091 mL
50 mM0.0353 mL0.1764 mL0.3527 mL1.7636 mL
100 mM0.0176 mL0.0882 mL0.1764 mL0.8818 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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

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