Pz-1|1800505-64-9|-陌孚医药/Medlife

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Pz-1

目录号: PL10973 纯度: ≥99%

CAS No. :1800505-64-9

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中文名称	Pz-1
中文别名	化合物 T12598
英文名称	Pz-1
英文别名	N-(5-(Tert-Butyl)isoxazol-3-yl)-2-(4-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)phenyl)acetamide;Pz-1;N-(5-tert-butyl-1,2-oxazol-3-yl)-2-[4-[5-(1-methylpyrazol-4-yl)benzimidazol-1-yl]phenyl]acetamide;NSC792733;Pz-1, >=98% (HPLC);PZ-1;Benzeneacetamide, N-[5-(1,1-dimethylethyl)-3-isoxazolyl]-4-[5-(1-methyl-1H-pyrazol-4-yl)-1H-benzimidazol-1-yl]-;Pz-1 >=98% (HPLC)
Cas No.	1800505-64-9
分子式	C₂₆H₂₆N₆O₂
分子量	454.52
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	Pz-1是有效地 RET 和 VEGFR2 受体酪氨酸激酶抑制剂，Pz-1抑制这两个野生型激酶的 IC₅₀ 值小于 1 nM。
生物活性	Pz-1 is a potent RET and VEGFR2 inhibitor with IC 50 s of less than 1 nM for both wild type kinases.
性状	Solid
IC50 & Target[1][2]	IC50: < 1 nM (RET and VEGFR2)
体外研究(In Vitro)	Pz-1 is a Type-II tyrosine kinase inhibitor, able to bind the DFG-out conformation of the kinase. In cell-based assays, 1.0 nM of Pz-1 strongly inhibits tyrosine phosphorylation of VEGFR2 and clinically relevant RET mutants, including those refractory to vandetanib and cabozantinib (RET and RET). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Pz-1 is shown active on VEGFR2, which can block blood supply required for RET-stimulated growth. At 1.0 mg/kg/day per os, Pz-1 abrogates formation of tumors induced by RET-mutant fibroblasts and blocks phosphorylation of both RET and VEGFR2 in tumor tissue. Pz-1 features no detectable toxicity up to 100.0 mg/kg, which indicates a large therapeutic window. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Frett B, et al. Fragment-Based Discovery of a Dual pan-RET/VEGFR2 Kinase Inhibitor Optimized for Single-Agent Polypharmacology. Angew Chem Int Ed Engl. 2015 Jul 20;54(30):8717-21.

溶解度数据	In Vitro: DMSO : 50 mg/mL (110.01 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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