Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2382 |
Vemurafenib
RO5185426,RG7204,维罗非尼,PLX4032 |
Raf; MAPK; ACK; Src; Autophagy | Angiogenesis; Autophagy; MAPK; Tyrosine Kinase/Adaptors |
Vemurafenib (RG7204) 是一种 B-RAF 抑制剂,可以抑制 RAFV600E 和 c-RAF-1 (IC50=31/48 nM),具有选择性和有效性。Vemurafenib 具有抗肿瘤活性,用于 BRAF V600E 突变阳性的黑色素瘤治疗。 | |||
T8654 |
Plx-4032
维罗非尼,Vemurafenib |
Raf | MAPK |
Plx-4032 (Vemurafenib) 是一种小分子 B-Raf 抑制剂,可用于治疗恶性黑色素瘤。 | |||
T27551 |
Honokiol DCA
Honokiol Bis-Dichloroacetate |
||
Honokiol DCA is an inhibitor of DRP1 phosphorylation. Honokiol DCA stimulates a phenotype suggestive of respiration through mitochondrial normalization and demonstrating activity in Vemurafenib-resistant melanoma in vivo. | |||
T27537 |
Hexafluoro
|
||
Hexafluoro is an inhibitor of DRP1 phosphorylation. Honokiol DCA stimulates a phenotype suggestive of respiration through mitochondrial normalization and demonstrates activity in Vemurafenib-resistant melanoma in vivo. | |||
T70424 | EBI-907 | ||
EBI-907 is a highly potent and orally efficacious B-RafV600E inhibitor. EBI-907 displays a low single-digit nanomolar activity (IC50 = 4.9 nM), which is >10-fold more potent than Vemurafenib (IC50 = 59 nM). EBI-907 also exhibits high potency in selectively inhibiting the proliferation of BRAF (V600E)-dependent cell lines (A375 and Colo205) and cellular Erk phosporylation, with superior activity to Vemurafenib. EBI-907, displaying potent activity against a number of important oncogenic kinases i... | |||
T78777 |
Vem-L-Cy5
|
Raf | MAPK |
Vem-L-Cy5 (化合物3)是一款改造自Vemurafenib的BRAF抑制剂, 其结构通过近红外荧光团Cy5进行修饰。该化合物针对BRAFV600E具有特异性,并能有效阻断MEK的磷酸化作用。Vem-L-Cy5展现了良好的细胞内渗透能力,并能抑制多种癌细胞系的生长。 | |||
T63210 | Everafenib | ||
Everafenib 是有效的、能够透过血脑屏障的 BRAF 抑制剂,对 MAPK 通路也具有抑制作用。Everafenib 能够抑制一系列 V600EBRAF 黑色素瘤细胞系的活性 (IC50: 2-10 nM),且效果比Dabrafenib 和Vemurafenib 好。Everafenib 可有效延长颅内转移性黑色素瘤小鼠模型的存活天数。 |