SCH772984

目录号: HY-50846 纯度: 98.97%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

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。

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SCH772984 Chemical Structure

CAS No. : 942183-80-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2044	In-stock
1 mg	￥719	In-stock
2 mg	￥1050	In-stock
5 mg	￥1438	In-stock
10 mg	￥2046	In-stock
25 mg	￥3376	In-stock
50 mg	￥4726	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 133 篇科研文献

: SCH772984 purchased from MCE. Usage Cited in: Nat Commun. 2023 Feb 13;14(1):802. [Abstract]; SCH772984 upregulates Mbp and Ng2, as well as significantly reduces Cd74 and Erk1/2, in primary neuronal cultures from control and Alzheimer’s disease knock-in mice (Fig. i and j).

: SCH772984 purchased from MCE. Usage Cited in: Acta Biomater. 2019 Feb;85:106-116. [Abstract]; Western analysis of related protein expression in the treatment of DBM/CBD-IKVAV-cRGD, DBM/CBD-IKVAV-cRGD + FAK inhibitor PF-573228 or DBM/CBD-IKVAV-cRGD + ERK inhibitor SCH772984.

: SCH772984 purchased from MCE. Usage Cited in: Sci Rep. 2019 Jan 29;9(1):907. [Abstract]; HCT116 cells are first treated with different concentrations of PD0325901 or SCH772984 for 36 h and are then treated without or with MG132 for 12 hours before harvested for analysis of the levels of proteins by western blotting using antibodies as indicated.

: SCH772984 purchased from MCE. Usage Cited in: Sci Rep. 2019 Jan 29;9(1):907. [Abstract]; KYSE70 cells are first treated with different concentrations of PD0325901 or SCH772984 for 36 hours and are then treated without or with MG132 for 12 hours before cells are harvested for western blotting using antibodies as indicated.

: SCH772984 purchased from MCE. Usage Cited in: Sci Rep. 2019 Jan 29;9(1):907. [Abstract]; HCT116 cells are treated with different concentrations of PD0325901 or SCH772984 before cells are harvested for western blotting analysis for ERK1/2 and phosphorylated ERK1/2

: SCH772984 purchased from MCE. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278. [Abstract]; BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM)+SCH772984 (10 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 6 h.

: SCH772984 purchased from MCE. Usage Cited in: Cancer Res. 2018 Feb 15;78(4):891-908. [Abstract]; A549 cells are treated with 10 μM SCH772984 (ERK1/2 inhibitor) or DMSO for 16 hr and analyzed for PSC formation by immunostaining

: SCH772984 purchased from MCE. Usage Cited in: J Immunol Res. 2018 Jun 7;2018:6249085. [Abstract]; The level of p-ERK1/2 expression is suppressed by SCH772984. RAW264.7 cells are preincubated with 1 μM SCH772984 for 2h followed by treatment with 20 μg/mL ox-LDL for 24 h.

: SCH772984 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Jan 1;495(1):781-786. [Abstract]; Representative images of migrated cells. HUVECs are pretreated with PD98059 (10 μM), SCH772984 (500 nM) or mock control for 2 h, and seeded in upper chambers of transwell inserts. VEGF (100 ng/ml), Scg3 (1 μg/ml) or PBS in medium with reduced FBS is added to bottom chambers in the presence or absence of the inhibitor. After culturing for 4 or 20 h, cells migrated to the lower surface of transwell membrane are stained with DAPI.

: SCH772984 purchased from MCE. Usage Cited in: J Neuroinflammation. 2017 Nov 25;14(1):228. [Abstract]; HSP70 release is reversed by ERK1/2 inhibitor in SH-SY5Y cells. SCH772984 (ERK1/2 inhibitor, 2 μM) is given 15 min. Supernatants are collected and analyzed by western blot (n=3).

: SCH772984 purchased from MCE. Usage Cited in: Neurotox Res. 2017 Nov;32(4):535-543. [Abstract]; Lithium promotes autophagy flux by activating MEK/ERK pathway in cells. Original Western blot showing LC3-II and p62 abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons. Arithmetic means±SEM (n=5) showing LC3-II abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons.

: SCH772984 purchased from MCE. Usage Cited in: Faculty of Medicine, Dentistry and Health Sciences. University of Melbourne. 2017 Sep.; Western blot analysis is performed on protein lysates from exponentially growing melanoma cell lines following 24 hours treatment with 0.1% DMSO as a vehicle control or: GSK1120212 (GSK212) 100 nM; GDC0623 100 nM or SCH772984 1 µM.

: SCH772984 purchased from MCE. Usage Cited in: Department of Dental Pharmacology. Okayama University. 2015.; The role of Semaphorin4D in bone invasion by oral cancer.

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ERK ERK1 ERK2 ERK5 ERK8

生物活性
纯度 & 产品资料
参考文献

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^[1].

IC₅₀ & Target^[1]

ERK2

1 nM (IC₅₀)

ERK1

4 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.004 μM Compound: SCH772984	Inhibition of ERK2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-ERK2 level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis Inhibition of ERK2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-ERK2 level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis	[PMID: 25977981]
A-375	IC₅₀	0.02 μM Compound: SCH772984	Inhibition of ERK1/2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-RSK level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis Inhibition of ERK1/2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-RSK level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis	[PMID: 25977981]
A-375	IC₅₀	0.07 μM Compound: SCH772984	Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant after 72 hrs by Cellomics ArrayScanTM VTI imaging analysis Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant after 72 hrs by Cellomics ArrayScanTM VTI imaging analysis	[PMID: 25977981]
A375-SM	IC₅₀	39 nM Compound: 1; SCH772984	Antiproliferative activity against human A375SM cells harboring BRAF V600E mutant measured after 96 hrs by Cell Titer-Glo assay Antiproliferative activity against human A375SM cells harboring BRAF V600E mutant measured after 96 hrs by Cell Titer-Glo assay	[PMID: 27329786]
COLO 205	IC₅₀	16 nM Compound: 5; SCH772984	Antiproliferative activity against human COLO205 cells harboring BRAF V600E/D mutant measured after 4 days Antiproliferative activity against human COLO205 cells harboring BRAF V600E/D mutant measured after 4 days	[PMID: 30034615]
HeLa	IC₅₀	> 50 μM Compound: 3; SCH772984	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs	[PMID: 32078308]
HL-60	IC₅₀	1.06 μM Compound: 3; SCH772984	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability measured after 24 hrs Antiproliferative activity against human HL60 cells assessed as reduction in cell viability measured after 24 hrs	[PMID: 32078308]
HT-29	IC₅₀	59 nM Compound: 5; SCH772984	Antiproliferative activity against human HT-29 cells harboring BRAF V600E/D mutant measured after 4 days Antiproliferative activity against human HT-29 cells harboring BRAF V600E/D mutant measured after 4 days	[PMID: 30034615]
HT-29	IC₅₀	96 nM Compound: 5; SCH772984	Induction of apoptosis in human HT-29 cells harboring BRAF/KRAS mutant by caspase activation assay Induction of apoptosis in human HT-29 cells harboring BRAF/KRAS mutant by caspase activation assay	[PMID: 29748051]
MKN-74	IC₅₀	> 50 μM Compound: 3; SCH772984	Antiproliferative activity against human MKN74 cells assessed as reduction in cell viability measured after 24 hrs Antiproliferative activity against human MKN74 cells assessed as reduction in cell viability measured after 24 hrs	[PMID: 32078308]

体外研究
(In Vitro)

SCH772984（300 nM；24-48 小时）导致 SCH772984 敏感黑色素瘤细胞出现 G1 停滞^[1]。
SCH772984（3-300 nM；24 小时）抑制 ERK 和 RSK 磷酸化^[1]。
SCH772984 在约 88% 和 49% 的 BRAF 突变体（n=25）或 RAS 突变体（n=35）肿瘤系中显示的 EC₅₀ 值低于 500 nM^[1]。

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

Cell Cycle Analysis^[1]

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^[1]

Cell Line:	LOX BRAF^V600E 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；腹腔注射；每天两次，持续 14 天）可使肿瘤消退 98%^[1]。
在 KRAS 突变型胰腺 MiaPaCa 模型中也观察到了剂量依赖性抗肿瘤活性，每天两次 50 mg/kg 剂量下肿瘤消退率为 36%。重要的是，肿瘤消退伴随着肿瘤组织中 ERK 磷酸化的强烈抑制。根据发病率、死亡率或体重减轻来衡量，SCH772984 在此给药方案下的耐受性良好^[1]。

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

Animal Model:	Female nude mice bearing human LOX BRAFV600E tumors^[1]
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).

分子量

587.67

Formula

C₃₃H₃₃N₉O₂

CAS 号

942183-80-4

性状

固体

颜色

Light yellow to yellow

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	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 30 mg/mL (51.05 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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

查看完整储备液配制表

* 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (5.10 mM); 澄清溶液

此方案可获得 ≥ 3 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

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); 澄清溶液
方案三

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); 悬浊液; 超声助溶

此方案可获得 1.43 mg/mL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。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案四

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 1.43 mg/mL (2.43 mM); 澄清溶液

此方案可获得 ≥ 1.43 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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。

方案一

请依序添加每种溶剂： 20% SBE-β-CD in Saline adjusted to pH 4-4.5 with 1 N Acetic
Solubility: 20 mg/mL (34.03 mM); 澄清溶液; 超声助溶
方案二

请依序添加每种溶剂： 50% PEG300 50% PBS
Solubility: 10 mg/mL (17.02 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 98.97%

选择批次：

Data Sheet (646 KB) SDS (252 KB)

COA (284 KB) HNMR (186 KB) LCMS (95 KB)

产品使用指南 (1538 KB)

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]

SCH772984 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7016 mL	8.5082 mL	17.0164 mL	42.5409 mL
	5 mM	0.3403 mL	1.7016 mL	3.4033 mL	8.5082 mL
	10 mM	0.1702 mL	0.8508 mL	1.7016 mL	4.2541 mL
	15 mM	0.1134 mL	0.5672 mL	1.1344 mL	2.8361 mL
	20 mM	0.0851 mL	0.4254 mL	0.8508 mL	2.1270 mL
	25 mM	0.0681 mL	0.3403 mL	0.6807 mL	1.7016 mL
	30 mM	0.0567 mL	0.2836 mL	0.5672 mL	1.4180 mL
	40 mM	0.0425 mL	0.2127 mL	0.4254 mL	1.0635 mL
	50 mM	0.0340 mL	0.1702 mL	0.3403 mL	0.8508 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SCH772984942183-80-4SCH 772984SCH-772984ERKExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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SCH772984

Customer Review

MCE 顾客使用本产品发表的 133 篇科研文献

SCH772984 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 ERK 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

SCH772984 相关分类

完整储备液配制表

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SCH772984

Customer Review

SCH772984 相关抗体

MCE 顾客使用本产品发表的 133 篇科研文献

SCH772984 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 ERK 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

SCH772984 相关抗体:

摩尔计算器

稀释计算器

SCH772984 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

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