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PLX7904

CAS No. : 1393465-84-3

MCE 站：PLX7904

产品活性：PLX7904 是有效的，选择性的 BRAF 抑制剂，在表达突变体 RAS 的细胞中，对 BRAF^V600E 的 IC₅₀ 值约为 5 nM。

研究领域：MAPK/ERK Pathway

作用靶点：Raf

In Vitro: PLX7904 inhibits the in vitro growth of two melanoma cell lines (A375 and COLO829) and an additional human colorectal cancer cell line COLO205 that expresses BRAF^V600E with IC₅₀ values of 0.17 μM, 0.53 μM, and 0.16 μM, respectively, on a par with vemurafenib IC₅₀ values in the same assays (0.33 μM, 0.69 μM, and 0.25 μM, respectively). PLX7904 and PLX8394 potently inhibit ERK1/2-driven GAL4-Elk1 reporter activity in PRT cells as well as parental cells. PLX7904 and PLX8394 treatment at 1 μM concentration reduce colony formation and viability in parental cells to a similar level as PLX4720. PPLX7904 potently inhibits phosphorylation of ERK1/2 in mutant BRAF melanoma cells without eliciting paradoxical activation in wild-type BRAF, mutant NRAS melanoma cells. PPLX7904 inhibits ERK1/2 in PLX470-resistant cell lines. PPLX7904 treatment promotes apoptosis and inhibits anchorage-independent growth of vemurafenib resistant cells.

相关产品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  MAPK Compound Library  |  Anti-Cancer Compound Library  |  Oxygen Sensing Compound Library  |  Ferroptosis Compound Library  |  Glutamine Metabolism Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Doramapimod  |  GW 5074  |  Ro 5126766  |  AZ 628  |  GDC-0879  |  ZM 336372  |  Agerafenib  |  Raf inhibitor 1  |  AZ304  |  L-779450  |  MCP110  |  Sorafenib (D3)  |  Raf inhibitor 2

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