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Refametinib (RDEA-119, BAY 86-9766)

MEK1/2 抑制剂

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产品目录号: A12866

库存状态:中国现货中国现货

产品名 目录号 价格 数量
Refametinib (RDEA-119, BAY 86-9766) 10mg A12866-10
¥ 2,140.00
Refametinib (RDEA-119, BAY 86-9766) 25mg A12866-25
¥ 2,900.00
Refametinib (RDEA-119, BAY 86-9766) 50mg A12866-50
¥ 5,990.00
Refametinib (RDEA-119, BAY 86-9766) 100mg A12866-100
¥ 10,260.00

产品仅用于研究,不针对患者销售,望谅解.

产品简介

Refametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity.

Refametinib (RDEA-119, BAY 86-9766)

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Chemical Information

目录号 A12866
Mechanism of action Inhibitor
分子量 572.34
化学分子式 C19H20F3IN2O5S
Solubility DMSO
纯度 >98%
储存方式 at -20°C 2 years
CAS No. 923032-38-6
Synonyms RDEA119, RDEA 119, BAY 86-9766, BAY 869766, BAY869766
SMILES code COC1=CC(=C(C(=C1NS(=O)(=O)C2(CC2)C[C@H](CO)O)NC3=C(C=C(C=C3)I)F)F)F
化学名称 N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide

生物活性

Description
Refametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity.

制备储备液

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 17.47 mL 87.36 mL 174.72mL
0.5 mM 3.49 mL 17.47 mL 34.94 mL
1 mM 1.75 mL 8.74 mL 17.47 mL
5 mM 0.35 mL 1.75 mL 3.49 mL

*The above data is based on the productmolecular weight 572.34. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Refametinib is a non–ATP-competitive inhibitor of MEK1/2. It inhibits MEK activity in an in vitro assay with IC50 values of 19nM and 47nM for MEK1 and MEK2, respectively. X-ray shows refametinib binds to an allosteric site of MEK. It does not affect ATP binding but precludes binding to the substrate ERK, thus preventing ERK phosphorylation. Refametinib inhibits MEK with EC50 values ranging from 2.5nM to 15.8nM in a variety of human cancer cells including A375, Colo205, HT-29 and MDA-MB-231. In addition, in the cancer cell lines harboring V600E BRAF mutant, refametinib suppresses cell growth with GI50 values ranging from 67nM to 89nM. Furthermore, in the human melanoma A375 tumor xenograft model, treatment of refametinib causes obvious tumor growth delay and regression. Refametinib also shows tumor growth inhibition in the xenograft model of human Colo205 tumor [1].

References:
[1] Iverson C, Larson G, Lai C, et al. RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer. Cancer research, 2009, 69(17): 6839-6847.

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