Elzovantinib (Synonyms: TPX-0022; CSF1R-IN-2)
目录号: PL11436 纯度: ≥99%
CAS No. :2271119-26-5
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中文名称
Elzovantinib
英文名称
Elzovantinib
英文别名
CSF1R-IN-2;TPX0022;NSC820832;elzovantinib;TTY12Q00LY;Elzovantinib [INN];TPX002;GTPL11869;s9620;compound 5 [WO2019023417A1]
Cas No.
2271119-26-5
分子式
C20H20FN7O2
分子量
409.42
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Elzovantinib (TPX-0022) 是 SRC,MET 和 c-FMS 的口服有效抑制剂, 其对 SRC,MET 和c-FMS 的 IC50 值分别为 0.12 nM,0.14 nM 和 0.76 nM。
生物活性
Elzovantinib (TPX-0022) is an oral-active inhibitor of SRC, MET and c-FMS, with IC 50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.
性状
Solid
IC50 & Target[1][2]
IC50: 0.12 nM (SRC), 0.14 nM (MET), 0.76 nM (c-FMS).
体外研究(In Vitro)
Elzovantinib (TPX-0022) causes the suppression of MET autophosphorylation as well as the downstream STAT3, ERK and AKT phosphorylation at IC50 values of around 1-3 nM in SNU-5 and MKN-45 cell lines. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Elzovantinib (TPX-0022; p.o., BID, 13 days) treatment results in an 85% tumor regression and no body weight loss is observed after 21 days treatment in mice.
Elzovantinib (p.o., BID, 10 days) demonstrates the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID and 15 mg/kg, BID, respectively in SCID/Beige mice.
Elzovantinib inhibits MET activity in MKN-45 tumors following oral administration in mice.
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
ClinicalTrial
参考文献
[1]. WO 2019023417 A1.
溶解度数据
In Vitro: DMSO : 25 mg/mL (61.06 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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