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抑制剂/激活剂

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凋亡与自噬

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SCH772984

SCH772984 是一种高选择性和 ATP 竞争性 ERK 抑制剂，对 ERK1 和 ERK2 的 IC50 分别为 4 和 1 nM。SCH772984 在对天然 MAPK 抑制和耐药 MAPK 抑制的细胞中的 BRAF 或 RAS 突变，具有抗肿瘤活性。

货号：
TK0386
规格：

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	942183-80-4
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-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.
分子式	C33H33N9O2
分子量	587.67
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 48 mg/mL (81.68 mM; Need ultrasonic)
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.
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.
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纯度及产品资料	98%

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