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SCH772984 TFA(free base)

目录号: PC11797 纯度: ≥98%

ERK1/2抑制剂,SCH772984 有效抑制 ERK1 和 ERK2 活性，IC50 分别为 4 和 1 nM。

CAS No. :942183-80-4

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中文名称

SCH772984 TFA(free base)

中文别名

(R)-1-(2--2-氧(4-(4-(嘧啶-2-基)苯基)对二氮己环-1-基)乙基)-N-(3-(吡啶-4-基)-1H--5INDAZOL-基)吡咯烷-3-甲酰胺;(R)-1-(2-氧代-2-(4-(4-(2-嘧啶L)苯基)-L-哌嗪)乙基)-3-[N-(3-(4-吡啶)吲唑-5-氨基]甲酰基-吡咯烷;SCH772984 抑制剂;(3R)-1-[2-氧代-2-[4-[4-(2-嘧啶基)苯基]-1-哌嗪基]乙基]-N-[3-(4-吡啶基)-1H-吲唑-5-基]-3-吡咯烷甲酰胺

英文名称

SCH772984 TFA(free base)

英文别名

(R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-yl)pyrrolidine-3-carboxamide;SCH772984;(3R)-1-[2-oxo-2-[4-(4-pyrimidin-2-ylphenyl)piperazin-1-yl]ethyl]-N-(3-pyridin-4-yl-1H-indazol-5-yl)pyrrolidine-3-carboxamide;(R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-yl)pyrrolidine-3-carboxami;SCH-772984;(3~{R})-1-[2-oxidanylidene-2-[4-(4-pyrimidin-2-ylphenyl)piperazin-1-yl]ethyl]-~{N}-(3-pyridin-4-yl-1~{H}-indazol-5-yl)pyrrolidine-3-carboxamide;(3r)-1-(2-Oxo-2-{4-[4-(Pyrimidin-2-Yl)phenyl]piperazin-1-Yl}ethyl)-N-[3-(Pyridin-4-Yl)-2h-Indazol-5-Yl]pyrrolidine-3-Carboxamide;38Z;GTPL8056;AOB6425;EX-

Cas No.

942183-80-4

分子式

C₃₃H₃₃N₉O₂

分子量

587.67

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

详情描述

ERK1/2抑制剂,SCH772984 有效抑制 ERK1 和 ERK2 活性，IC50 分别为 4 和 1 nM。

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.

性状

Solid

IC50 & Target[1][2]

ERK2

1 nM (IC₅₀)

ERK1

4 nM (IC₅₀)

体外研究(In Vitro)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis

Cell Line:	LOX cells (SCH772984-sensitive melanoma cells)
Concentration:	300 nM
Incubation Time:	24, 48 hours
Result:	Revealed a G1 arrest as well as an increase in the sub-G1 fraction indicative of apoptosis.

Western Blot Analysis

Cell Line:	LOX BRAF melanoma cells
Concentration:	3, 10, 30, 100, 300 nM
Incubation Time:	24 hours
Result:	A dose-dependent inhibition of phosphorylation of the ERK substrate RSK (T359/S363 phospho-RSK), and also inhibited phosphorylation of residues in the activation loop of ERK itself (T202/Y204 and T185/Y187 of ERK1 and ERK2, respectively).

体内研究(In Vivo)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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).

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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. [Information]

溶解度数据

体外研究:

DMSO : 48 mg/mL (81.68 mM; Need ultrasonic)

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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.

建议依照次序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.4 mg/mL (4.08 mM); Clear solution
3.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.43 mg/mL (2.43 mM); Clear solution

此方案可获得 ≥ 1.43 mg/mL (2.43 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
4.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 1.43 mg/mL (2.43 mM); Suspended solution; Need ultrasonic

此方案可获得 1.43 mg/mL (2.43 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
5.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.43 mg/mL (2.43 mM); Clear solution

此方案可获得 ≥ 1.43 mg/mL (2.43 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

搜索质检报告(COA)

产品使用指南

Data Sheet

[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. [Information]

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。

SCH772984 TFA(free base)

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