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BI-4142

Catalog No. T63643Cas No. 2682003-36-5

BI-4142 is an orally active, potent and selective HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling.

BI-4142

BI-4142

Purity: 98.09%
Catalog No. T63643Cas No. 2682003-36-5
BI-4142 is an orally active, potent and selective HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling.
Pack SizePriceAvailabilityQuantity
1 mg$226In Stock
5 mg$562In Stock
10 mg$883In Stock
25 mg$1,450In Stock
50 mg$1,980In Stock
1 mL x 10 mM (in DMSO)$645In Stock
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Purity:98.09%
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Product Introduction

Bioactivity
Description
BI-4142 is an orally active, potent and selective HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling.
Targets&IC50
Ba/F3 EGFRWT:2400 nM, HEK HER2YVMA:10 nM, HEK EGFRWT:270 nM, Ba/F3 HER2YVMA:18 nM, HER2:5 nM
In vitro
BI-4142 inhibits HER2-dependent cell lines and downstream signaling, with IC50 values of 10 nM, 18 nM, 270 nM, and 2400 nM against HEK HER2YVMA, Ba/F3 HER2YVMA, HEK EGFRWT, and Ba/F3 EGFRWT, respectively[1].BI-4142 (1 nM-5 μM, 72 h or 96 h) exhibits antiproliferative activity against tumor cells[1].
In the CaCo-2 assay, BI-4142 displays good permeability and no PgP-mediated efflux liability[1].
In vivo
BI-4142 administered at doses ranging from 0 to 100 mg/kg, orally twice daily for 40 days, significantly inhibits tumor growth and suppresses oncogenic signaling[1].
Chemical Properties
Molecular Weight521.57
FormulaC28H27N9O2
Cas No.2682003-36-5
Storage & Solubility Information
StorageShipping with blue ice.
Solubility Information
DMSO: 80 mg/mL (153.38 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9173 mL9.5864 mL19.1729 mL95.8644 mL
5 mM0.3835 mL1.9173 mL3.8346 mL19.1729 mL
10 mM0.1917 mL0.9586 mL1.9173 mL9.5864 mL
20 mM0.0959 mL0.4793 mL0.9586 mL4.7932 mL
50 mM0.0383 mL0.1917 mL0.3835 mL1.9173 mL
100 mM0.0192 mL0.0959 mL0.1917 mL0.9586 mL

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