Vemurafenib (PLX4032, RG7204)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Vemurafenib是BRAF激酶的抑制剂，它可以抑制突变型BRAF V600E的活性，同时也可以抑制CRAF、ARAF和野生型BRAF激酶的活性。Vemurafenib是一个竞争性的小分子抑制剂，针对丝氨酸-苏氨酸激酶，靶向结合突变型BRAF的ATP结合域。在无BRAF突变的细胞中，Vemurafenib可以增强由RAF同源或异源二聚体对下游MEK的激活，这是由于在BRAF-CRAF异源二聚体和CRAF-CRAF同源二聚体中非药物结合伴侣的反式激活引起的。
参考文献：
Keith. T Flaherty, Uma Yasothan and Peter Kirkpatrick. Vemurafenib. Nature Reviews Drug Discovery. 2011; 10: 811 – 812.
Jason J. Luke, F. Stephen Hodi. Vemurafenib and BRAF Inhibition: A New Class of Treatment for Metastatic Melanoma. Clinical Cancer Research. 2012; 18: 9 – 14.
- 1. MENGTING OU, XICHAO XU, et al. "MDM2 induces EMT via the B‑Raf signaling pathway through 14‑3‑3." Oncol Rep. 2021 Jul;46(1):120. PMID:33955525
- 2. Satoh TK, Mellett M, et al. "IL-36γ drives skin toxicity induced by EGFR/MEK inhibition and commensal Cutibacterium acnes." J Clin Invest. 2019 Dec 5. pii: 128678. PMID:31805013
- 3. Sechi M, Lall RK, et al. "Fisetin targets YB-1/RSK axis independent of its effect on ERK signaling:insights from in vitro and in vivo melanoma models." Sci Rep. 2018 Oct 24;8(1):15726. PMID:30356079
- 4. Zanconato F, Battilana G, et al. "Transcriptional addiction in cancer cells is mediated by YAP/TAZ through BRD4." Nat Med. 2018 Oct;24(10):1599-1610. PMID:30224758
- 5. Hwang BJ, Adhikary G, et al. "Chk1 inhibition as a novel therapeutic strategy in melanoma." Oncotarget. 2018 Jul 13;9(54):30450-30464. PMID:30100999
- 6. Talebi A, Dehairs J, et al. "Sustained SREBP-1-dependent lipogenesis as a key mediator of resistance to BRAF-targeted therapy." Nat Commun.2018 Jun 27;9(1):2500. PMID:29950559
- 7. Zuo Q, Liu J, et al. "AXL/AKT axis mediated-resistance to BRAF inhibitor depends on PTEN status in melanoma."Oncogene. 2018 Mar 19. PMID:29551771
- 8. Fisher ML, Grun D, et al. "Inhibition of YAP function overcomes BRAF inhibitor resistance in melanoma cancer stem cells." Oncotarget.2017 Nov 22;8(66):110257-110272. PMID:29299145
- 9. Sieber J, Wieder N, et al. "GDC-0879, a BRAF(V600E) Inhibitor, Protects Kidney Podocytes from Death." Cell Chem Biol. 2017 Dec 6. PMID:29249695
- 10. Basu R, Baumgaertel N, et al. "Growth Hormone Receptor Knockdown Sensitizes Human Melanoma Cells to Chemotherapy by Attenuating Expression of ABC Drug Efflux Pumps. Horm Cancer." 2017 Jun;8(3):143-156. PMID:28293855
- 11. Yuan He, Djoke Hendriks, et al. "Melanoma-directed activation of apoptosis using a novel bispecific antibody directed at MCSP and TRAIL receptor 2/Death Receptor 5." Journal of Investigative Dermatology,February 2016, volume 136, pages 541-4.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 489.93 |
| Cas No. | 918504-65-1 |
| Formula | C23H18ClF2N3O3S |
| Synonyms | Vemurafenib,Zelboraf,PLX-4032,RG7204,RO5185426, |
| Solubility | ≥24.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | N-[3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl]propane-1-sulfonamide |
| SDF | Download SDF |
| Canonical SMILES | CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=NC=C(C=C23)C4=CC=C(C=C4)Cl)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验： | |
|
细胞系 |
MALME-3M黑色素瘤细胞系 |
|
溶解方法 |
在DMSO中的溶解度 >10 mM。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应时间 |
24 h；10 μM |
|
应用 |
在黑色素瘤细胞系中，RG7204在表达BRAF V600E而非BRAF WT的细胞中有效抑制细胞增殖。RG7204也有效抑制表达其它密码子600 BRAF突变（V600D、V600 K和V600R）的黑色素瘤细胞的增殖。 |
| 动物实验： | |
|
动物模型 |
无胸腺裸鼠 |
|
剂量 |
100 mg/kg；口服给药。 |
|
应用 |
在Colo829肿瘤异种移植小鼠中，RG7204以100 mg/kg的剂量口服给药21天，在肿瘤细胞植入后第38天研究结束时，与对照相比，RG7204极大提高了抗肿瘤活性（P = 0.001）。所有10只RG7204处理的小鼠均出现完全的肿瘤消退，其存活率与对照相比也显著提高（P = 0.0008）。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Yang H, Higgins B, Kolinsky K, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models[J]. Cancer research, 2010, 70(13): 5518-5527. |
|
| 描述 | Vemurafenib (PLX4032, RG7204)是一种新型有效的B-Raf V600E抑制剂，IC50值为31 nM。 | |||||
| 靶点 | B-RafV600E | C-Raf | MAP4K5 (KHS1) | SRMS | ACK1 | FGR |
| IC50 | 31 nM | 48 nM | 51 nM | 18 nM | 19 nM | 63 nM |
质量控制和MSDS
- 批次：
化学结构
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