Pz-1 |CAS:1800505-64-9 Probechem Biochemicals

Chemical Structure : Pz-1

CAS No.: 1800505-64-9

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Pz-1 (RET inhibitor Pz-1)

货号: PC-61163Not For Human Use, Lab Use Only.

Pz-1 is a potent, dual pan-RET/VEGFR2 kinase inhibitor with IC50s of <1 nM for all RET, RET V804M and VEGFR2.

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10 mg	￥980	In stock
25 mg	￥1580	In stock
50 mg	￥2580	In stock
100 mg		Get quote

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生物&药学活性

Pz-1 is a potent, dual pan-RET/VEGFR2 kinase inhibitor with IC50s of <1 nM for all RET, RET V804M and VEGFR2.
Pz-1 displays good global kinase selectivity with only 7 kinases against a 91 kinase panel at 50 nM, strongly inhibites phosphorylation of RET and mutant RET oncoproteins at 1 nM in cell-based assays, inhibits RETC634Y NIH3T3 fibroblast proliferation with IC50 of 0.5 nM.
Pz-1 abrogates the formation of tumors induced by RET-mutant fibroblasts and blocks the phosphorylation of both RET and VEGFR2 in tumor tissue at 1.0 mg/kg without detectable toxicity.

物理化学性质&存储条件

分子量	454.534
分子式	C26H26N6O2
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	N-(5-(tert-butyl)isoxazol-3-yl)-2-(4-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)phenyl)acetamide

参考文献

1. Frett B, et al. Angew Chem Int Ed Engl. 2015 Jul 20;54(30):8717-21.

Pz-1 (RET inhibitor Pz-1)

生物&药学活性

物理化学性质&存储条件

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Pz-1 (RET inhibitor Pz-1)

生物&药学活性

物理化学性质&存储条件

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