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BI-4142

Chemical Structure : BI-4142

CAS No.: 2682003-36-5

BI-4142 (BI 4142)

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.

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10 mg $398 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 521.57
Formula C28H27N9O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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]-

References

1. To C, et al. Nat Cancer. 2022 Apr;3(4):402-417.

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