CEP-32496
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.
CEP-32496是一种高效的和口服有效的BRAF突变体V600E、野生型BRAF和c-Raf抑制剂，Kd值分别为14 nM、36 nM和39 nM。
除了BRAF（V600E）之外，CEP-32496对野生型BRAF和相关的CRAF表现出高的结合亲和力，对某些可以用于疾病治疗的受体酪氨酸激酶，如Abl-1、c-Kit、RET、PDGFR- β和VEGFR-2也具有结合能力。CEP-32496对于MAPK信号转导途径的RAF成员具有选择性，但是对MAPK通路的其他关键激酶没有显著亲和力，包括MEK-1、MEK-2、ERK-1和ERK-2。这表明，观察到的细胞活性主要是通过抑制BRAF（V600E）驱动的。与表达野生型BRAF的肿瘤细胞系相比，CEP-32496对表达BRAF突变体的肿瘤细胞系具有选择性的细胞毒性[1]，这个实验结果进一步支持了上述论点。
在Colo-205肿瘤异种移植小鼠中，口服给药CEP-32496，显著抑制了肿瘤细胞裂解物中的pMEK[1]。
参考文献：
[1] Rowbottom MW1,Faraoni R,Chao Q,Campbell BT,Lai AG,Setti E,Ezawa M,Sprankle KG,Abraham S,Tran L,Struss B,Gibney M,Armstrong RC,Gunawardane RN,Nepomuceno RR,Valenta I,Hua H,Gardner MF,Cramer MD,Gitnick D,Insko DE,Apuy JL,Jones-Bolin S,Ghose AK,Herbertz T,Ator MA,Dorsey BD,Ruggeri B,Williams M,Bhagwat S,James J,Holladay MW. Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro
-2-methylpropan- 2-yl) isoxazol-3-yl) urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E. J Med Chem.2012 Feb 9;55(3):1082-105. doi: 10.1021/jm2009925. Epub 2012 Jan 23.
| Storage | Store at -20°C |
| M.Wt | 517.46 |
| Cas No. | 1188910-76-0 |
| Formula | C24H22F3N5O5 |
| Solubility | ≥25.85 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | 1-[3-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-3-[5-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-3-yl]urea |
| SDF | Download SDF |
| Canonical SMILES | CC(C)(C1=CC(=NO1)NC(=O)NC2=CC(=CC=C2)OC3=NC=NC4=CC(=C(C=C43)OC)OC)C(F)(F)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。 |
质量控制和MSDS
- 批次:
化学结构
