Bezuclastinib (CGT9486, PLX9486)

Chemical Structure : Bezuclastinib

CAS No.: 1616385-51-3

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货号: PC-73407Not For Human Use, Lab Use Only.

Bezuclastinib (CGT9486, PLX9486) is a potent, selective tyrosine kinase inhibitor (TKI) targeting mutated KIT and demonstrating potent activity in vitro against primary exon 9 and 11 mutations, as well as secondary exon 17 and 18 mutations.

规格	价格	库存
5 mg	￥3280	In stock
10 mg	￥5280	In stock
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100 mg		Get quote

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生物&药学活性

Bezuclastinib (CGT9486, PLX9486) is a potent, selective tyrosine kinase inhibitor (TKI) targeting mutated KIT and demonstrating potent activity in vitro against primary exon 9 and 11 mutations, as well as secondary exon 17 and 18 mutations.
Bezuclastinib (CGT9486, PLX9486) is a potent inhibitor of growth and KIT phosphorylation in the imatinib-sensitive and imatinib-resistant BaF3 cell lines, with growth IC50=61 nM for KIT-WT and more potently against BaF3 KIT p.D816V (IC50=6.6 nM) and BaF3 KIT p.V560G/D816V (IC50=7.1 nM).
Bezuclastinib (CGT9486, PLX9486) demonstrated signifcant tumor regression and strong inhibition of MAPK activation in imatinib-resistant GIST patient-derived xenograft (PDX) models.

物理化学性质&存储条件

分子量	331.379
分子式	C19H17N5O
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	4,5-dimethyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazole-3-carboxamide

参考文献

1. Gebreyohannes YK, et al. Clin Exp Med. 2019 May;19(2):201-210.

2. Wagner AJ, et al. JAMA Oncol. 2021 Sep 1;7(9):1343-1350.