产品
编 号：F282826
分子式：C20H20FN7O2
分子量：409.42
分子式：C20H20FN7O2
分子量：409.42
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 2271119-26-5
产品详情
生物活性：
Elzovantinib (TPX-0022) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.
体内研究：
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.Animal Model:Mice bearing LU2503 tumors patient derived xenograft (PDX) NSCLC model.
Dosage:15 mg/kg.
Administration:PO, BID (twice daily) for 13 days.
Result:Resulted in an 85% tumor regression and no body weight loss was observed after 21 days treatment.
Animal Model:SCID/Beige mice bearing Ba/F3 ETV6-CSF1R tumors with average tumor size of ~180 mm3.
Dosage:5 and 15 mg/kg.
Administration:PO, BID (twice daily) for 10 days.
Result:Demonstrated the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID and 15 mg/kg, BID, respectively.
体外研究：
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.
Elzovantinib (TPX-0022) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.
体内研究：
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.Animal Model:Mice bearing LU2503 tumors patient derived xenograft (PDX) NSCLC model.
Dosage:15 mg/kg.
Administration:PO, BID (twice daily) for 13 days.
Result:Resulted in an 85% tumor regression and no body weight loss was observed after 21 days treatment.
Animal Model:SCID/Beige mice bearing Ba/F3 ETV6-CSF1R tumors with average tumor size of ~180 mm3.
Dosage:5 and 15 mg/kg.
Administration:PO, BID (twice daily) for 10 days.
Result:Demonstrated the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID and 15 mg/kg, BID, respectively.
体外研究：
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.
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