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BMS-599626 Hydrochloride

🥰Excellent
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

🥰Excellent
Purity: 100%
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 SizePriceAvailabilityQuantity
1 mg$37In Stock
5 mg$87In Stock
10 mg$133In Stock
25 mg$253In Stock
50 mg$447In Stock
100 mg$659In Stock
1 mL x 10 mM (in DMSO)$109In Stock
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Purity:100%
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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, HER2:32nM, HER4:190 nM
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].
AliasAC480 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.
Solubility Information
DMSO: 90.0 mg/mL (158.7 mM), Sonication is recommended.
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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