保存条件 ：4℃

保质期 ：详见说明

英文名 ：SCH772984

库存 ：充足

供应商 ：杭州昊鑫生物

CAS号 ：942183-80-4

规格 ：2mg

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。

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[1].

体外研究
SCH772984 (300 nM; 24-48hours) results in a G1 arrest in SCH772984-sensitive melanoma cells[1].
SCH772984 (3-300 nM; 24 hours) inhibits ERK and RSK phosphorylation[1].
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[1].

体内研究
SCH772984 (12.5-50 mg/kg; i.p.; twice daily for 14 days) leads to 98% tumor regression[1].
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[1].

分子量    
587.67

性状    
Solid

Formula    
C33H33N9O2

CAS 号    
942183-80-4

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
In solvent    -80°C    6 months
-20°C    1 month
溶解性数据    
In Vitro: 
DMSO : 48 mg/mL (81.68 mM; Need ultrasonic)

配制储备液    
浓度溶剂体积质量    1 mg    5 mg    10 mg
1 mM    1.7016 mL    8.5082 mL    17.0164 mL
5 mM    0.3403 mL    1.7016 mL    3.4033 mL
10 mM    0.1702 mL    0.8508 mL    1.7016 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： 20% SBE-β-CD adjusted to pH 4-4.5 with 1 N acetic

Solubility: 20 mg/mL (34.03 mM); Clear solution; Need ultrasonic

2.
请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

Solubility: ≥ 2.4 mg/mL (4.08 mM); Clear solution

3.
请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

Solubility: ≥ 1.43 mg/mL (2.43 mM); Clear solution

4.
请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

Solubility: 1.43 mg/mL (2.43 mM); Suspended solution; Need ultrasonic

5.
请依序添加每种溶剂： 10% DMSO    90% corn oil

Solubility: ≥ 1.43 mg/mL (2.43 mM); Clear solution
 

参考文献	[1]. Morris EJ, et al. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discov. 2013 Jul;3(7):742-50.  [Content Brief]