BI-4142

Modify Date: 2024-01-05 22:50:47

BI-4142 structure	Common Name	BI-4142
	CAS Number	2682003-36-5	Molecular Weight	521.57
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₈H₂₇N₉O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of BI-4142

BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM[1].

Name	BI-4142

Description	BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> EGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
Target	HER2:5 nM (IC50)
In Vitro	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[1]. BI-4142 (1 nM-5 μM, 72 h or 96 h) shows antiproliferative activity against tumor cells[1]. BI-4142 displays good permeability and no PgP-mediated efflux liability in the CaCo-2 assay[1]. BI-4142 inhibits HER2-dependent cell lines and inhibits downstream signaling[1]. Cell Proliferation Assay[1] Cell 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.
In Vivo	BI-4142 (0-100 mg/kg; p.o.; twice per day for 40 days) inhibits tumor growth and inhibits oncogenic signaling[1]. Animal Model: NMRI-Foxn1nu mice, PC-9 HER2YVMA xenograft model[1] 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[1] 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 (Pharmacokinetic Analysis) Result: In vivo mouse PK data for BI-4142[1] Compound Dose iv/po (mg/kg) tmax (h) Cmax (nM) AUD (h•nM) Plasma CL (mL/min/kg) % F i.v., 1mg/kg n/a n/a 3,280 9.69 n/a BI-4142 p.o., 10 mg/kg 0.83 8,600 23,200 n/a 71 p.o., 100 mg/kg 0.67 36,400 196,000 n/a 60
References	[1]. Wilding B, et al. Discovery of potent and selective HER2 inhibitors with efficacy against HER2 exon 20 insertion-driven tumors, which preserve wild-type EGFR signaling. Nat Cancer. 2022 Jul;3(7):821-836.

Molecular Formula	C₂₈H₂₇N₉O₂
Molecular Weight	521.57

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: BI-4142
Price: Negotiable
Purity: 98.09%
Delivery: 10 Day
Contact: Huang
Email: sales@echemcloud.com

DC Chemicals Limited
China
Product Name: BI-4142
Price: ￥800.0/100mg ￥3360.0/250mg ￥6720.0/1g
Purity: 98.0%
Delivery: 10 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

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