Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T63855 |
B-Raf IN 6
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B-Raf IN 6 是蛋白激酶 B-Raf 的有效抑制剂 (IC50: 1.7 nM)。B-Raf IN 6 不结合二级靶点 PXR,并可抵抗快速代谢。B-Raf IN 6 对癌症疾病表现出研究潜力。 | |||
T10299 |
AMG PERK 44
|
PERK; Autophagy | Apoptosis; Autophagy |
AMG PERK 44 是一种具有口服活性和选择性的 PERK 抑制剂(IC50:6 nM),可诱导自噬。AMG PERK 44 抑制 GCN2(IC50:7300 nM)和 B-Raf(IC50 >1000 nM),可用于研究癌症。 | |||
T79572 |
MAPK-IN-2
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
MAPK-IN-2 (化合物3h)是一种携带抗肿瘤活性的高效MAPK抑制剂。它在多个癌细胞系中有效抑制了细胞增殖,并对MAPK途径表现出强大的抑制效果(EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT IC50=112 nM, CDK4/6 IC50=95和184 nM),对突变型EGFR和B-RAF亦展现出高效力(EGFRT790M IC50=69 nM, B-RAFV600E IC50=83 nM)。 | |||
T36676 |
Rineterkib hydrochloride
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Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer[1]. ERK-IN-1 (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the C... |