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  • 维罗非尼|T2382|TargetMol

维罗非尼|T2382|TargetMol

Vemurafenib
918504-65-1
￥262 5mg 起订
￥430 10mg 起订
￥690 25mg 起订
上海 更新日期：2024-12-02

TargetMol中国（陶术生物）

VIP12年
联系人：邵小姐
电话：021-021-33632979拨打
手机：15002134094 拨打
邮箱：marketing@targetmol.com

产品详情:

中文名称：
维罗非尼
英文名称：
Vemurafenib
CAS号：
918504-65-1
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.65%
产品类别：
抑制剂
货号：
T2382

Product Introduction

Bioactivity

名称Vemurafenib
描述Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31/48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.
细胞实验Cellular proliferation was evaluated by MTT assay. Briefly, cells were plated in 96-well microtiter plates at a density of 1,000 to 5,000 cells per well in a volume of 180 μL. For the assay, RG7204 was prepared at 10 times the final assay concentration in media containing 1% DMSO. Twenty-four hours after cell plating, 20 μL of the appropriate dilution were added to plates in duplicate. The plates were assayed for proliferation 6 days after the cells were plated according to the procedure originally described by Mosmann [2].
激酶实验Expression and purification of B-RAF, structure determination, and protein kinase activity measurements were carried out as previously described. To obtain co-crystals of B-RAFV600E with PLX4032, the protein solution was initially mixed with the compound dissolved in DMSO at a final compound concentration of 1 mM. This complex was co-crystallized by a sitting drop vapor diffusion experiment in which equal volumes of complex (at 10 mg/ml concentration) and reservoir solution (100mM BisTris at pH 6.0, 12.5% 2,5-hexanediol, and 12% PEG3350) were mixed and allowed to equilibrate against the reservoir at 4°C. The crystal was soaked in cryosolvent, followed by flash-freezing in liquid nitrogen. The data were collected at Beamline ALS831 with the wavelength of 1.11?. The Ramachandran plot from the refined structure shows that 94%, 5.6% and 0.4% residues are in the most favored, additional allowed and generously allowed regions, respectively. A summary of the crystallography statistics is included in Supplementary Table 3. COLO205 tumor xenograft studies (Molecular Imaging Research, Ann Arbor, MI) were carried out as previously described either using a conventional formulation (5%DMSO, 1% methylcellulose) or using the MBP formulation [1].
动物实验All animal procedures were approved by the Ethical Commission of the Institute for Cancer Research and Treatment and by the Italian Ministry of Health. WiDr cells were injected subcutaneously into the right posterior flanks of 7-week-old immunodeficient NODSCID female mice (6 mice per group). Tumour formation was monitored twice a week, and tumour volume based on caliper measurements was calculated by the modified ellipsoidal formula: tumour volume = 1/2 length × width. When tumours reached a volume of approximately 200–250 mm^3, mice were randomly assigned to treatment with vehicle or drug(s) [3].
体外活性方法：黑色素瘤细胞 A375 和 SK-Mel-28 用 Vemurafenib (0-8 μM) 处理 48 h，使用 CCK-8 assay 检测细胞活力。 结果：Vemurafenib 剂量依赖性抑制 A375 和 SK-Mel-28 细胞增殖，IC50 分别为 0.8 μM 和 1.8 μM。[1] 方法：表达 BRAF V600E 的黑色素瘤细胞系 Colo829 和 LOX 用 Vemurafenib (0.05-30 μmol/L) 处理 2 h，使用 Western Blot 方法检测靶点蛋白表达水平。 结果：Vemurafenib 抑制了 Colo829 和 LOX 细胞中 MEK 和 ERK 的磷酸化。[2]
体内活性方法：为检测体内抗肿瘤活性，将 Vemurafenib (12.5-75 mg/kg，suspended in an aqueous vehicle containing 2% Klucel LF and adjusted to pH 4 with dilute HCl.) 口服给药给携带黑色素瘤 LOX 的 Athymic nude 小鼠，每天两次，持续 11-13 天。 结果：Vemurafenib 显著抑制肿瘤生长并诱导肿瘤消退。[2] 方法：为检测体内抗肿瘤活性，将 Vemurafenib (60 mg/kg) 口服给药给携带黑色素瘤 Colo-205 的 athymic mice 小鼠，每天两次，持续十四天。 结果：Vemurafenib 有效抑制 Colo-205 异种移植小鼠模型中的肿瘤生长。[3]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 9 mg/mL (18.37 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 18.33 mg/mL (37.42 mM), Sonication is recommended.
关键字Raf kinases | PLX 4032 | inhibit | RG 7204 | PLX-4032 | Inhibitor | RO-5185426 | Vemurafenib | Raf | RG-7204 | Autophagy | RO 5185426 | 1029872-54-5
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维罗非尼|||RO5185426|||RG7204|||PLX4032|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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