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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
RO4987655, 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
RO4987655 is an orally active and highly selective MEK inhibitor with an IC 50 of 5.2 nM for inhibition of MEK1 / MEK2 .
In Vitro
RO4987655 potently inhibits mitogen-activated protein kinase signaling pathway activation and tumor cell growth, with an in vitro IC 50 of 5.2 nM for inhibition of MEK1/2. RO4987655 inhibits proliferation of NCI-H2122 cells in a dose-dependent manner with an IC 50 value of 0.0065 μM. RO4987655 at doses ranging from 0.1 to 1.0 μM suppresses pERK1/2 already at 2 h after the start of treatment. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Single-agent oral administration of RO4987655 (CH4987655) results in complete tumor regressions in xenograft models. RO4987655 is rapidly absorbed with a t max of ~1 h. Exposures are dose proportional from 0.5 to 4 mg. The disposition is biphasic with a terminal t 1/2 of ~25 hr. Intersubject variability is low, 9% to 23% for C max and 14% to 25% for area-under-the-curve (AUC). pERK inhibition is exposure dependent and is greater than 80% inhibition at higher doses. The pharmacokinetic-pharmacodynamic relationship is characterized by an inhibitory E max model (E max ~100%; IC 50 40.6 ng/mL) using nonlinear mixed-effect modeling . Female athymic nude mice are randomized into study groups. The tumors size is estimated with digital caliper and PET scans performed on days 0, 1, and 3 with 1.0, 2.5, and 5.0 mg/kg RO4987655. The vehicle treatment does not inhibit the NCI-H2122 tumor xenograft growth over this time frame. In contrast, RO4987655 treatment results in 119% tumor growth inhibition (TGI) at 1.0 mg/kg, 145% TGI at 2.5 mg/kg and 150% TGI at 5.0 mg/kg on day 3. PET imaging shows that [ 18 F] FDG uptake in the xenografts decreases within 24 h (day 1) from the administration of RO4987655. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
The human lung adenocarcinoma cell line NCI-H2122 are maintained in the designated media and indicated concentrations of heat-inactivated fetal bovine serum and L-glutamine. Cells are grown at 37°C in an atmosphere of 5%CO 2 . Cells are treated with various concentrations of RO4987655 (0.00001, 0.001, 0.1, and 10 μM) for 72 h in 96-well plates and viable cells were quantified with Cell Counting Kit-8. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal administration
Mice Female athymic nude mice Balb nu/nu , age 5 to 6 weeks (18 to 22 g) are used. NCI-H2122 cells (4×10 6 /mouse) are inoculated subcutaneously in the right flank of Balb-nu/nu mice. Once tumors are established (100 to 200 mm 3 ), mice are randomized into groups with similar mean tumor volumes at the start of the study. The tumors size is estimated with digital caliper and PET scans performed on days 0, 1, and 3 with 1.0, 2.5, and 5.0 mg/kg RO4987655 . Tumor volume and body weight are measured on days 0 (baseline), 1, 2, 3, and 9 of [18F] FDG-PET imaging. Tumor growth inhibition is calculated . aladdin has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:MEK1 5.2 nM (IC 50 ) MEK2 5.2 nM (IC 50 )
规格
规格或纯度
Moligand™, 10mM in DMSO
英文名称
RO4987655
生化机理
RO4987655 是一种口服活性高选择性 MEK 抑制剂，抑制 MEK1 / MEK2 的 IC 50 为 5.2 nM。
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
C1CC(=O)N(OC1)CC2=CC(=C(C(=C2F)F)NC3=C(C=C(C=C3)I)F)C(=O)NOCCO
PubChem CID
分子量
565.29
技术文档
高级数据
产品属性
| ALogP | 3 |
|---|
关联靶点（人）
MAP2K2
Tclin
双特异性丝裂原活化蛋白激酶激酶 2(Dual specificity mitogen-activated protein kinase kinase 2)
(0 活性数据)
MAPK1
Tchem
丝裂原活化蛋白激酶1(Mitogen-activated protein kinase 1)
(0 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)
(0 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
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