![N-[(2S)-2,3-二羟基丙基]-3-[(2-氟-4-碘苯基)氨基]-4-吡啶甲酰胺, 双特异性丝裂原活化蛋白激酶激酶 2 抑制剂](https://www.aladdin-e.com/media/catalog/product/cache/207e23213cf636ccdef205098cf3c8a3/P/4/P408137.png)
计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
N-[(2S)-2,3-二羟基丙基]-3-[(2-氟-4-碘苯基)氨基]-4-吡啶甲酰胺, 双特异性丝裂原活化蛋白激酶激酶 2 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Pimasertib (AS-703026) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines.A potent inhibitor of MEK1 and MEK2.
Information
Pimasertib (AS-703026, MSC1936369B, SAR 245509) is a highly selective, potent, ATP non-competitive allosteric inhibitor ofMEK1/2withIC50of 5 nM-2 μM in MM cell lines. Phase 2.
In vitro
AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor that binds to the distinctive MEK allosteric site and therefore exhibits exquisite kinase selectivity. AS703026 inhibits growth and survival of human multiple myeloma (MM) cells, including U266 and INA-6, with IC50 of 5 nM and 11 nM, respectively. Such an inhibitory effect by AS703026 is mediated by G0-G1 cell cycle arrest and is accompanied by reduced expresson of the MAF oncogene. AS703026 further induces apoptosis via caspase-3 and PARP cleavage in MM cells, both in the presence or absence of bone marrow stromal cells (BMSCs). AS703026 may be an effective therapy in colorectal cancer caused by K-Ras mutation. AS703026 (10 μM) effectively inhibits the ERK pathway, proliferation, and transformation in human DLD-1 colorectal cancer cells what carry a mutant allele of K-Ras (D-MUT).
In vivo
AS703026 (15 and 30 mg/kg) significantly inhibits tumor growth in a human plasmacytoma xenograft model of H929 MM cells. This can be correlated with downregulated pERK1/2, induced PARP cleavage, and decreased microvessels. AS703026 (10 mg/kg) inhibits tumor growth, and markedly decreases p-ERK level in a xenograft mouse model of human K-Ras mutated (D-MUT) colorectal tumor.
Cell Data
cell lines：
Concentrations：2 nM - 20 μM (stock: 10 mM in DMSO)
Incubation Time：48 hours
Powder Purity:≥97%
规格
英文别名
MSC1936369B, SAR 245509 | (S)-N-(2,3-dihydroxypropyl)-3-(2-fluoro-4-iodophenylamino)isonicotinamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Pimasertib (AS-703026)
生化机理
Pimasertib（AS-703026，MSC1936369B，SAR 245509）是一种高选择性、强效、ATP 非竞争性的 MEK1/2 异位抑制剂，在 MM 细胞系中的 IC50 为 5 nM-2 μM。第二阶段
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
双特异性丝裂原活化蛋白激酶激酶 2 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1=CC(=C(C=C1I)F)NC2=C(C=CN=C2)C(=O)NC[C@@H](CO)O
分子量
431.2
Reaxy-Rn
40713281
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=40713281&ln=
技术文档
高级数据
关联靶点（人）
IARS2
Tchem
异亮氨酸--tRNA连接酶，线粒体(Isoleucine--tRNA ligase, mitochondrial)
(1 活性数据)
MAP2K1
Tclin
双特异性丝裂原活化蛋白激酶激酶 1(Dual specificity mitogen-activated protein kinase kinase 1)
(3 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 48 mg/mL (196.52 mM); Ethanol: 48 mg/mL (196.52 mM); Water: Insoluble;
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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