TAK-632
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.
TAK-632是BRAF、CRAF和BRAF-V600E激酶的选择性抑制剂,IC50分别为8.3 nM、1.4 nM和2.4 nM[1]。
RAF激酶含有三种亚型的丝氨酸/苏氨酸特异性蛋白激酶家族,在RAS-RAF-MEK-ERK信号转导级联中发挥重要作用,参与促分裂原活化蛋白激酶(MAPK)级联反应[2]。
TAK-632是一种有效的pan-RAF激酶抑制剂,与已报道的pan-RAF激酶抑制剂vemurafenib相比具有更高的选择性。在SK-MEL-2细胞中,TAK-632以剂量依赖性方式诱导BRAF-CRAF二聚体形成。在黑色素瘤细胞系A375和SK-MEL-2中,TAK-632具有显著抗增殖作用,GI50值分别为6 nom/L和11 nom/L [1]。
在SK-MEL-2皮下异种移植小鼠模型中,口服剂量为60或120 mg/kg/d的TAK-632,每天一次,服用21天,显著减少磷酸化ERK和肿瘤生长,并且没有严重毒性[1] 。
有研究表明,TAK-632是pERK的有效抑制剂,IC50为25 nM[1]。
参考文献:
[1]. Nakamura, A., et al., Antitumor activity of the selective pan-RAF inhibitor TAK-632 in BRAF inhibitor-resistant melanoma. Cancer Res, 2013. 73(23): p. 7043-55.
[2]. Korkut, A., et al., Perturbation biology nominates upstream-downstream drug combinations in RAF inhibitor resistant melanoma cells. Elife, 2015. 4.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 554.52 |
Cas No. | 1228591-30-7 |
Formula | C27H18F4N4O3S |
Solubility | ≥27.75 mg/mL in DMSO; insoluble in H2O; ≥2.23 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | N-[7-cyano-6-[4-fluoro-3-[[2-[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide |
SDF | Download SDF |
Canonical SMILES | C1CC1C(=O)NC2=NC3=C(S2)C(=C(C=C3)OC4=CC(=C(C=C4)F)NC(=O)CC5=CC(=CC=C5)C(F)(F)F)C#N |
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。 |
Description | TAK-632是Raf的有效抑制剂,对B-Raf和C-Raf的IC50分别为8.3 nM和1.4 nM。 | |||||
靶点 | B-Raf | C-Raf | ||||
IC50 | 8.3 nM | 1.4 nM |
质量控制和MSDS
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