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蚂蚁淘在线 / 品牌中心 / Selleck Chemicals / Selleck Chemicals/Refametinib (RDEA119)/S1089

Selleck Chemicals/Refametinib (RDEA119)/S1089

价格
￥1940.00
货号：S1089
浏览量：127
品牌：Selleck Chemicals
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商品描述
DescriptionRefametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.
Targets
MEK1 [1](Cell-free assay)MEK2 [1](Cell-free assay)
19 nM47 nM
In vitro

RDEA119 is selectively bound directly to an allosteric pocket in the MEK1/2 enzymes, and highly efficacious at inhibiting cell proliferation in several tumor cell lines, including A375, SK-MEI-28, Colo205, HT-29 and BxPC3. RDEA119 inhibits anchorage-dependent growth of human cancer cell lines harboring the gain-of-function V600E BRAF mutant with GI50 values ranging from 67 to 89 nM. Under anchorage-independent conditions, GI50 values for all cell lines tested are similar (40-84 nM). RDEA119 shows a tissue selectivity that reduces its potential for central nervous system–related side effects. [1] RDEA119 potently inhibits the proliferation of the 4 cell lines that harbored BRAF mutation but has no or modest effects on the other 4 cells that harbored wild-type BRAF (IC50 of 0.034-0.217 μM vs. 1.413-34.120 μM). This inhibitory effect of RDEA119 in selected cell lines OCUT1 (BRAF V600E(+), PIK3CA H1047R(+)) and SW1376 (BRAF V600E(+)) is enhanced by combination with the mTOR inhibitor, temsirolimus. RDEA119 and temsirolimus also show synergistic effects on autophagic death of OCUT1 and KAT18 cells selectively tested. [2]

Assay
MethodsTest IndexPMID
Growth inhibition assay
IC50;

PubMed: 29896883

Cell proliferation assays of a panel of 26 CRC cell lines. Cells were exposed to increasing concentrations of refametinib for 72 h and evaluated for proliferation by MTT assays.

29896883
Western blot
p-BRAF / BRAF / p-MEK / MEK / p-ERK / ERK ;

PubMed: 29896883

Western blot analyses of downstream effector proteins of the MAPK signaling pathway. The panel of CRC cell lines was treated with or without refametinib (1 lM) for 72 h. a-Tubulin served as a loading control.

Cyclin D1 / Cyclin E / p27 ;

PubMed: 29896883

Western blot analyses of cell cycle effector proteins in CRC cell lines after treatment with refametinib (0, 0.1, and 1 μM) for 72 h. a-Tubulin served as a loading control.

p-STAT3 / STAT3 ;

PubMed: 29896883

KRAS mutant CRC cell lines were treated with or without refametinib (1 lM) for 48 h. p-STAT3 and total STAT3 levels were determined by western blotting. a-Tubulin served as a loading control.

29896883
In vivoOral administration of RDEA119 at 50 mg/kg on a once daily × 14 schedule leads to a 68% tumor growth inhibition (TGI) in human melanoma A375 tumor model. Oral administration of RDEA119 at 25 mg/kg on a once a once daily × 14 schedule leads to a 123% TGI in human colon carcinoma Colo205 tumor model (TGI > 100% occurs when the tumor shrinks below its starting volume). A dose of 25 mg/kg once daily × 14 produces 56% and 67% TGI for HT-29 and A431 tumors, respectively. [1]
Selleck Chemicals一直专注于生命科学领域高端试剂的开发与研究，旨在以最优价格为客户提供最优质的科研试剂服务。我们的产品包括抗体，重组蛋白，干扰rna，多肽，小分子激酶抑制剂等。Selleck Chemicals拥有一支热情与活力并存，经验与技术兼备的技术支持与客户服务团队，凭借在生命科学领域的多年研发经验，公司与多达2万多个客户建立了长期稳定的合作关系，其中包括世界各大制药厂，生物科技公司，医院及各大临床诊断实验室，世界各著名高校、研究所以及政府机关。