MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

LY3009120

CAS No. : 1454682-72-4

MCE 站：LY3009120

产品活性：LY3009120 (DP-4978) 是泛 RAF 抑制剂，其抑制BRAF^V600E，BRAF^WT 和CRAF^WT 的 IC₅₀ 分别为 5.8，9.1和15 nM。

研究领域：MAPK/ERK Pathway  |  Autophagy

作用靶点：Raf  |  Autophagy

In Vitro: In the whole-cell based KiNativ assay, LY3009120 shows affinity to each RAF isoform with the IC₅₀ of 44, 31-47 ａnd 42 nM for ARAF, BRAF ａnd CRAF respectively. LY3009120 exhibits anti-proliferative effects on cell lines harboring BRAF^V600E, KRAS^G13 ａnd KRAS^G12 mutations. LY3009120 (1 μM) inhibits the phosphorylation of both MEK1/2 ａnd ERK1/2 in cell lines with high basal levels of pMEK1/2 ａnd pERK1/2 (RKO ａnd HCT 116). LY3009120 shows inhibitory effect on tumor cells such as BxPC-3, NCI-H2405 ａnd OV-90 cell lines. LY3009120 (0.01 μM) demonstrates potent ａnd dose-dependent inhibition of phospho-MEK ａnd ERK in all three cell lines. LY3009120 demonstrates a concentration-dependent cell growth inhibition with IC₅₀ values of 0.04, 0.087, ａnd 0.007 μM against H2405, BxPC-3, ａnd OV-90 cells, respectively. LY3009120 inhibits BRAF^WT, CRAF^WT, BRAF^V600E, ａnd BRAF^V600E+G468A with the IC₅₀ values of 9.1, 15, 5.8, ａnd 17 nM, respectively. LY3009120 induces BRAF-CRAF dimerization but inhibits the phosphorylation of downstream MEK ａnd ERK. LY3009120 also inhibits various forms of RAF dimers including BRAF or CRAF homodimers. LY3009120 gives only very minor activation at very low doses, with near complete inhibition of phospho-ERK at concentrations above 100 nM.

In Vivo: LY3009120 (20 mg/kg bid) displays significant activity in in vivo BRAF^mut ａnd KRAS^mut CRC xenograft models. In Colo 205 xenografts (BRAF^mut), LY3009120 results in statistically significant tumor regression, while treatment of HCT 116 xenografts (KRAS^mut) results in statistically significant inhibition of tumor growth. LY3009120 treatment reduces pMEK1/2 in all HT-29 xenografts ａnd reduces pERK1/2 in the majority of HT-29 xenografts. LY3009120 (15 or 30 mg/kg) achieves almost complete tumor growth regression, ａnd inhibits downstream phospho-MEK ａnd ERK by approximately 70% ａnd 60%, respectively, in the H2405 model.

相关产品：Covalent Screening Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  MAPK Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Autophagy Compound Library  |  Covalent Screening Library  |  Oxygen Sensing Compound Library  |  Ferroptosis Compound Library  |  Glutamine Metabolism Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Sorafenib  |  Vemurafenib  |  Dabrafenib  |  Regorafenib  |  Encorafenib  |  Doramapimod  |  PLX-4720  |  GW 5074  |  Ro 5126766  |  Belvarafenib  |  AZ 628  |  LXH254  |  GDC-0879  |  Lifirafenib  |  RAF265  |  TAK-580  |  SB-590885  |  TAK-632  |  BI-882370  |  RAF709  |  ZM 336372  |  PLX7904  |  Agerafenib  |  PROTAC B-Raf degrader 1  |  AD80  |  BRAF inhibitor

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。