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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > MAPK > CobimetinibCAS：934660-93-2
Molecular Formula：C21H21F3IN3O2
Molecular Weight：531.31
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 934660-93-2 |
| Name | Cobimetinib |
| Molecular Formula | C21H21F3IN3O2 |
| Molecular Weight | 531.31 |
| Solubility | Soluble in DMSO ≥10mg/mL |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD22124461 |
| SMILES | OC1([C@H]2NCCCC2)CN(C1)C(C3=C(C(F)=C(C=C3)F)NC4=C(C=C(C=C4)I)F)=O |
| Target Point | MEK |
| Passage | MAPK |
| Background | Cobimetinib is a potent and highly selective MEK1 inhibitor |
| Biological Activity | 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。[1-2] |
| In Vitro | Cobimetinib对一组广泛类型的肿瘤细胞的生长表现出强烈的抑制活性，特别是对BRAF或KRAS突变型癌细胞系。结合GDC-0941，GDC-0973在888MEL和A2058细胞中导致生存能力降低，通路抑制，以及细胞凋亡增加。[1] GDC-0973和vemurafenib联合给药显著增加所有BRAFV600E系中细胞膜上减少的GLUT-1水平。[2] |
| In Vivo | 在负荷BRAFV600E和KRAS突变型肿瘤的小鼠体内，Cobimetinib(10 mg/kg，p.o.)产生抗肿瘤作用，结合GDC-0973和GDC-0941能够提高疗效。[1]在负荷耐药的A375异种移植物小鼠体内，GDC-0973与GDC-0941结合诱导己糖激酶II，c-RAF，Ksr 和p-MEK蛋白质的水平减少。[2] |
| Data Literature Source | [1] Hoeflich KP，et al. Cancer Res. 2012，72(1)，210-219. [2] Baudy AR，et al. EJNMMI Res. 2012，2(1)，22. |
| Unit | Bottle |
| Specification | 2mg 5mg |
是一种有效的高选择性MEK1抑制剂
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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