| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| C408172-1ml |
1ml |
现货  |
|
| 英文别名 | RG7420 | [3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl][3-hydroxy-3-(2S)-2-piperidinyl-1-azetidinyl]-methanone |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Cobimetinib (GDC-0973) |
| 生化机理 | Cobimetinib（GDC-0973，RG7420）是一种强效、高选择性的 MEK1 抑制剂，IC50 为 4.2 nM，对 MEK1 的选择性是 MEK2 的 100 倍以上。Cobimetinib 可诱导细胞凋亡。第 3 阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 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 |
| 产品介绍 |
(GDC-0973, RG7420)是一种有效的高选择性MEK1抑制剂，IC50 为 4.2 nM。其对MEK1的选择性比对MEK2高100倍以上，对其他很多丝氨酸-苏氨酸和酪氨酸激酶没有显著抑制作用。Cobimetinib 可诱导凋亡。 Cobimetinib是丝裂原活化蛋白激酶激酶（MEK）选择性抑制剂,其IC50值为0.9 nM。 MEK是一种激酶，选择性磷酸化丝氨酸/苏氨酸和酪氨酸残基，并参与丝裂原活化蛋白激酶（MAPK）信号转导通路，从而调控细胞增殖、存活、分化、移动和血管生成。 在同时携带KRAS G13D和B-RAF G464V突变的MDA-MB-231T乳腺癌细胞中，Cobimetinib抑制MEK，其IC50值为0.2 nM。在药代动力学-药效学（PK-PD）模型中， Cobimetinib在肿瘤内的停留时间比在血浆中更长，显示出持续的持续的肿瘤药效学应答。 在WM-266-4异种移植小鼠中，Cobimetinib可以减少肿瘤中的pERK，其IC50值分别为0.78 mM（WM-266-4）和0.52 mM。此外，Cobimetinib（3.89 mM）增加WM-266-4小鼠的IC50值。在A375异种移植物小鼠中，Cobimetinib（0.3 ~ 30 mg/kg）呈剂量依赖性地抑制肿瘤。目前，Cobimetinib作为一种潜在的抗肿瘤剂，正处于I期临床试验。 Information Cobimetinib (GDC-0973, RG7420) is a potent and highly selectiveMEK1inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threoni Cobimetinib shows strong activity on cell growth inhibtion in a broad panel of tumor types, particularly in BRAF or KRAS mutant cancer cell lines. In combination with GDC-0941, GDC-0973 results in reduced viability, pathway inhibition, and increased apoptosis in 888MEL and A2058 cells. Coadministration of GDC-0973 and vemurafenib significantly increases decreased levels of GLUT-1 on the cellular membrane across all BRAFV600E lines. In vivo In mice bearing BRAFV600E and KRAS mutant tumors, Cobimetinib (10 mg/kg, p.o.) produces antitumor efficacy, and the combination of GDC-0973 and GDC-0941 show improved efficacy. In mice bearing drug-resistant A375 xenografts, combination of GDC-0973 and GDC-0941 induces decreased levels of hexokinase II, c-RAF, Ksr and p-MEK protein. cell lines：U-937, HL-60, KG-1, HNT-34 and GDM-1 Concentrations： Incubation Time： Powder Purity:≥99% |
| IC50 | MEK1, IC50: 4.2 nM |
|---|---|
| ALogP | 3.701 |
| hba_count | 1 |
| HBD Count | 2 |
| Rotatable Bond | 4 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | OC1(CN(C1)C(=O)C2=C(NC3=CC=C(I)C=C3F)C(=C(F)C=C2)F)C4CCCCN4 |
| 分子量 | 531.31 |
| Reaxy-Rn | 26026088 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26026088&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 49 mg/mL (200.58 mM); Ethanol: 49 mg/mL (200.58 mM); Water: Insoluble; |
|---|---|
| DMSO(mg / mL) Max Solubility | 100 |
| DMSO(mM) Max Solubility | 188.21 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 26026088 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26026088&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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