ChemicalBook CAS DataBase List 2681392-19-6

2681392-19-6

Name	BI-1622
CAS	2681392-19-6
Molecular Formula	C26H24N10O2
Molecular Weight	508.53
MOL File	2681392-19-6.mol

Chemical Properties

density	1.46±0.1 g/cm3(Predicted)
form	Solid
pka	3.24±0.30(Predicted)
color	Light yellow to yellow

Hazard Information

Uses

BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile[1].

in vivo

BI-1622 (1 mg/kg, IV; 10 and 100 mg/kg, Orally; once) shows moderate clearance, a moderate volume of distribution, and good to moderate bioavailability^[1].
BI-1622 (0-100?mg/kg, orally, twice daily) inhibits tumor growth and inhibits oncogenic signaling in vivo^[1].

Animal Model:	Female NMRI-Foxn1nu mice (6-8 weeks old, 8-10 mice per cage, engrafted subcutaneously with PC-9 HER2YVMA, NCI-H2170 HER2YVMA or NCI-N87 cells)^[1]
Dosage:	10, 30 and 100?mg/kg
Administration:	orally, twice daily
Result:	In the NCI-H2170 HER2YVMA mechanistic model, 100?mg/kg twice daily BI-1622 resulted in a delay in tumor growth (73% TGI). In the ST3107 HER2 exon 20 mutant model, both BI-4142 (100?mg/kg twice daily) resulted in tumor regressions.

Animal Model:	NMRI Foxn1nu mice (n=3 per group)^[1]
Dosage:	1 mg/kg (IV); 10 and 100 mg/kg (Orally)
Administration:	IV, Orally; once (Pharmacokinetic Analysis)
Result:	Showed moderate in vivo clearance (50% hepatic blood flow), a moderate volume of distribution, and good to moderate bioavailability of up to 68%.

IC 50

HER2: 7 nM (IC₅₀); ErbB4; EGFR; CDK11B; JAK3

References

[1] Lamarre L, 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. DOI:10.1038/s43018-022-00412-y

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