产品
编 号：F531465
分子式：C33H33N9O2
分子量：587.67
分子式：C33H33N9O2
分子量：587.67
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
1635
In-stock
1mg
575
In-stock
2mg
840
In-stock
5mg
1150
In-stock
10mg
1637
In-stock
25mg
2701
In-stock
50mg
3781
In-stock
100mg
5294
In-stock
结构图
CAS No: 942183-80-4
产品详情
生物活性：
SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-na?ve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.
体内研究：
SCH772984 (12.5-50 mg/kg; i.p.; twice daily for 14 days) leads to 98% tumor regression.Dose-dependent antitumor activity is also observed in the KRAS-mutant pancreatic MiaPaCa model, with 36% regression at 50 mg/kg twice daily. Importantly, tumor regression is accompanied by robust inhibition of ERK phosphorylation in tumor tissue. SCH772984 is well tolerated on this schedule as measured by morbidity, lethality, or body weight loss.Animal Model:Female nude mice bearing human LOX BRAFV600E tumors
Dosage:12.5, 25, 50 mg/kg
Administration:Intraperitoneal injection; twice daily for 14 days
Result:Tumor regressions were observed at all doses, such as 17% at 12.5 mg/kg, 84% at 25 mg/kg, and 98% at 50 mg/kg).
体外研究：
SCH772984 (300 nM; 24-48hours) results in a G1 arrest in SCH772984-sensitive melanoma cells.SCH772984 (3-300 nM; 24 hours) inhibits ERK and RSK phosphorylation.SCH772984 shows EC50 values less than 500 nM in approximately 88% and 49% of BRAF-mutant (n=25) or RAS-mutant (n=35) tumor lines, respectively.
SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-na?ve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.
体内研究：
SCH772984 (12.5-50 mg/kg; i.p.; twice daily for 14 days) leads to 98% tumor regression.Dose-dependent antitumor activity is also observed in the KRAS-mutant pancreatic MiaPaCa model, with 36% regression at 50 mg/kg twice daily. Importantly, tumor regression is accompanied by robust inhibition of ERK phosphorylation in tumor tissue. SCH772984 is well tolerated on this schedule as measured by morbidity, lethality, or body weight loss.Animal Model:Female nude mice bearing human LOX BRAFV600E tumors
Dosage:12.5, 25, 50 mg/kg
Administration:Intraperitoneal injection; twice daily for 14 days
Result:Tumor regressions were observed at all doses, such as 17% at 12.5 mg/kg, 84% at 25 mg/kg, and 98% at 50 mg/kg).
体外研究：
SCH772984 (300 nM; 24-48hours) results in a G1 arrest in SCH772984-sensitive melanoma cells.SCH772984 (3-300 nM; 24 hours) inhibits ERK and RSK phosphorylation.SCH772984 shows EC50 values less than 500 nM in approximately 88% and 49% of BRAF-mutant (n=25) or RAS-mutant (n=35) tumor lines, respectively.
产品资料
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