上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
Vemurafenib (Synonyms: 维罗非尼; PLX4032; RG7204; RO5185426) 纯度: 99.83%
Vemurafenib (PLX4032; RG7204; RO5185426) 是首创的,有效的 B-RAF 选择性抑制剂,能够抑制 RAFV600E 和 c-RAF-1 的活性,IC50 分别为 31 nM 和 48 nM。Vemurafenib 可以诱导细胞自噬 (autophagy)。
Vemurafenib Chemical Structure
CAS No. : 918504-65-1
规格 | 价格 | 是否有货 | 数量 |
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥567 | In-stock | |
10 mg | ¥515 | In-stock | |
50 mg | ¥1300 | In-stock | |
100 mg | ¥2300 | In-stock | |
200 mg | ¥4100 | In-stock | |
500 mg | ¥6890 | In-stock | |
1 g | ¥11500 | In-stock | |
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10 g | 询价 |
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Vemurafenib 相关产品
•相关化合物库:
- Drug Repurposing Compound Library Plus
- FDA-Approved Drug Library Plus
- FDA-Approved Drug Library Mini
- Bioactive Compound Library Plus
- Immunology/Inflammation Compound Library
- Kinase Inhibitor Library
- MAPK Compound Library
- FDA-Approved Drug Library
- Anti-Cancer Compound Library
- Autophagy Compound Library
- Drug Repurposing Compound Library
- Oxygen Sensing Compound Library
- Ferroptosis Compound Library
- Orally Active Compound Library
- Glutamine Metabolism Compound Library
- FDA Approved & Pharmacopeial Drug Library
- Anti-Lung Cancer Compound Library
- Drug-Induced Liver Injury (DILI) Compound Library
- Anti-Pancreatic Cancer Compound Library
- Targeted Therapy Drug Library
- Anti-Liver Cancer Compound Library
- Rare Diseases Drug Library
- Anti-Colorectal Cancer Compound Library
生物活性 |
Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5]. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
Vemurafenib (PLX4032) selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells[1]. RG7204 is a potent inhibitor of proliferation in those expressing RAFV600E but not BRAFWT in 17 melanoma cell lines. Vemurafenib (RG7204) induces MEK and ERK phosphorylation at high concentrations in CHL-1 cells[2]. Ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Vemurafenib (PLX4032, 20, 25, 75 mg/kg, p.o.) causes dose-dependent inhibition of tumor growth, with higher exposures resulting in tumor regression of BRAF mutant xenografts[1]. RG7204 (12.5, 25, and 75 mg/kg, p.o.) significantly inhibits tumor growth and induced tumor regression in mice bearing LOX tumor xenografts[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
489.92 |
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Formula |
C23H18ClF2N3O3S |
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CAS 号 |
918504-65-1 |
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中文名称 |
维罗非尼;维罗菲尼;威罗菲尼;唯罗非尼 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 50 mg/mL (102.06 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [2] |
Briefly, cells are 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, Vemurafenib (RG7204) is 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 are added to plates in duplicate. The plates are assayed for proliferation 6 days after the cells are plated according to the procedure. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [2] |
Athymic nude mice, are with ages 13 to 14 weeks, and weighing approximately 23 to 25 g. For the LOX xenografts, 2×106 cells in 0.2 mL of PBS are injected s.c. into the right lateral flank. Vemurafenib (RG7204), formulated as MBP, is suspended at the desired concentration as needed for each dose group in an aqueous vehicle containing 2% Klucel LF and adjusted to pH 4 with dilute HCl. NSC 362856 is of 250-mg capsules. Capsules are opened and combined into one bulk supply. To prepare the stock dosing material, NSC 362856 is first dissolved in 100% DMSO followed by dilution with saline to form a final milky white suspension in 10% DMSO/90% saline (pH 3.4). 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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