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Chemical Structure : BI-4142
CAS No.: 2682003-36-5
Catalog No.: PC-49226Not For Human Use, Lab Use Only.
BI-4142 (BI 4142) is a potent, selective, covalent and orally active HER2 inhibitor with IC50 of 5 nM, potently inhibits HER2 exon 20 mutants while sparing WT EGFR.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $258 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $588 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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BI-4142 (BI 4142) is a potent, selective, covalent and orally active HER2 inhibitor with IC50 of 5 nM, potently inhibits HER2 exon 20 mutants while sparing WT EGFR.
BI-4142 (5 uM) inhibits the proliferation of HER2-dependent cell lines 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.
BI-4142 dose-dependently decreases pHER2 and pERK levels in NCI-H2170 HER2YVMA and PC-9 HER2YVMA cells.
BI-4142 inhibits tumor growth and inhibits oncogenic signaling in preclinical xenograft models of HER2 exon 20 mutant non-small cell lung cancer.
| M.Wt | 521.57 | |
| Formula | C28H27N9O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-Propen-1-one, 1-[4-[8-[[3-methyl-4-[(1-methyl-1H-benzimidazol-5-yl)oxy]phenyl]amino]pyrimido[5,4-d]pyrimidin-2-yl]-1-piperazinyl]- |
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1. To C, et al. Nat Cancer. 2022 Apr;3(4):402-417.
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