BI-4142

Research use only, not for human use.

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 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM.

BI-4142 shows inhibition 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 (1 nM-5 μM, 72?h or 96?h) shows antiproliferative activity against tumor cells.BI-4142 displays good permeability and no PgP-mediated efflux liability in the CaCo-2 assay.BI-4142 inhibits HER2-dependent cell lines and inhibits downstream signaling.Cell Proliferation AssayCell Line:NCI-H2170 HER2WT, NCI-H2170 HER2YVMA, A431 EGFRWT, Ba/F3 HER2YVMA, Ba/F3 HER2YVMA,S783C, Ba/F3 EGFRWT and Ba/F3 EGFRC775S cells Concentration:1 nM-5 μM Incubation Time:72?h or 96?h Result:Showed antiproliferative effect with IC50 values of 16 nM, 82 nM, >5?μM, 4 nM, 24 nM, 718 nM and 43 nM against NCI-H2170 HER2WT, NCI-H2170 HER2YVMA, A431 EGFRWT, Ba/F3 HER2YVMA, Ba/F3 HER2YVMA,S783C, Ba/F3 EGFRWT and Ba/F3 EGFRC775S, respectively.

BI-4142 (0-100 mg/kg; p.o.; twice per day for 40 days) inhibits tumor growth and inhibits oncogenic signaling.Animal Model:NMRI-Foxn1nu mice, PC-9 HER2YVMA xenograft model Dosage:3, 10, 30 and 100 mg/kg Administration:Oral administration, twice per day for 40 days Result:Resulted in tumor regressions in a dose-dependent manner (113%, 126%, 153% and 166% tumor growth inhibition at 3, 10, 30 and 100 mg/kg, respectively).Animal Model:BomTac:NMRI Foxn1nu mice Dosage:1 mg/kg or 10mg/kg and 100 mg/kg Administration:IV for 1 mg/kg, PO for 10mg/kg and 100 mg/kg.

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Angiogenesis

HER/HSP

HER

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2682003-36-5

521.57

C28H27N9O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (191.73 mM; Ultrasonic )

O=C(C=C)N1CCN(C2=NC=C3N=CN=C(NC4=CC=C(OC=5C=CC6=C(N=CN6C)C5)C(=C4)C)C3=N2)CC1

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(-20℃)

With Ice Pack

≥ 2 years