JBJ-08-178-01 | HER2 inhibitor | Probechem Biochemicals

Chemical Structure : JBJ-08-178-01

CAS No.: 2401867-58-9

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JBJ-08-178-01 (HER2 inhibitor)

货号: PC-38578Not For Human Use, Lab Use Only.

JBJ-08-178-01 is a potent, selective and covalent HER2 inhibitor with IC50 of 2.21 nM and 7.04 nM for HER2 WT and EGFR WT, targets multiple HER2 activating mutations, including exon 20 insertions as well as amplification (IC50 values<50 nM).

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2 mg	￥2580	In stock
5 mg	￥4580	In stock
10 mg	￥7280	In stock
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100 mg		Get quote

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生物&药学活性

JBJ-08-178-01 is a potent, selective and covalent HER2 inhibitor with IC50 of 2.21 nM and 7.04 nM for HER2 WT and EGFR WT, targets multiple HER2 activating mutations, including exon 20 insertions as well as amplification (IC50 values<50 nM).
JBJ-08-178-01 maintained potency against non-insertion mutations, including S310F, L755S, V777L, V842I, and exon 19 indel (755_757LREdelinsRP) of HER2.
JBJ-08-178-01 exhibited a much greater degree of HER2-selectivity in Ba/F3 cell lines than in biochemical assays, owing to weak growth inhibition against Ba/F3 cells with WT EGFR (IC50=368 nM).
JBJ-08-178-01 showed strong antitumoral activity in HER2- mutant or amplified cancers in vitro and in vivo.
Treatment with JBJ-08-178-01 also led to a reduction in total HER2 by promoting proteasomal degradation of the receptor.
JBJ-08-178-01 is a selective, dual-action inhibitor and destabilizer of HER2 with potential efficacy and tolerance against NSCLC harboring HER2 genetic alterations or amplification.

物理化学性质&存储条件

分子量	562.634
分子式	C31H30N8O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(E)-N-(4-((4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide

参考文献

1. Jieun Son, et al. Cancer Res. 2022 Apr 15;82(8):1633-1645.

JBJ-08-178-01 (HER2 inhibitor)

生物&药学活性

物理化学性质&存储条件

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JBJ-08-178-01 (HER2 inhibitor)

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