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B-Raf IN 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
B-Raf IN 1图片
CAS NO:950736-05-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 515.53
Formula C29H24F3N5O
CAS No. 950736-05-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 53 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES O=C(NC1=CC=CC(C2=CC=NC3=C(C4=CC=C(CN(C)C)C=C4)C=NN23)=C1)C5=CC=CC(C(F)(F)F)=C5
Synonyms B-Raf-IN-1; B-Raf-IN 1; B-Raf-IN1
实验参考方法
In Vitro

In vitro activity: B-Raf IN 1 is a novel, potent and selective B-Raf inhibitor with IC50 of 24 nM; it is equally potent against c-Raf with IC50 of 25 nM. Moderate selectivity was observed for compound 10n versus p38a (IC50: 0.216 lM) and CAMKII (IC50: 0.822 lM), while high selectivity was observed versus CDK2, CDK4, PKCa, IKKb, JNK1, MK2, PKA, Src, MKK6, PLK1, p70S6K, PI3 Ka, and PDK1 (IC50s:>2 lM). It binds to B-Raf kinase without forming a hinge-binding hydrogen bond. With basic amine residues appended to C-3 aryl residues, cellular activity and solubility were enhanced over previously described compounds of this class.


Kinase Assay: B-Raf IN 1 is a novel, potent and selective B-Raf inhibitor with IC50 of 24 nM; it is equally potent against c-Raf with IC50 of 25 nM. Moderate selectivity was observed for compound 10n versus p38a (IC50: 0.216 lM) and CAMKII (IC50: 0.822 lM), while high selectivity was observed versus CDK2, CDK4, PKCa, IKKb, JNK1, MK2, PKA, Src, MKK6, PLK1, p70S6K, PI3 Ka, and PDK1 (IC50s:>2 lM). It binds to B-Raf kinase without forming a hinge-binding hydrogen bond. With basic amine residues appended to C-3 aryl residues, cellular activity and solubility were enhanced over previously described compounds of this class.


Cell Assay:

In Vivo
Animal model
Formulation & Dosage
References Bioorg Med Chem Lett. 2009 Dec 1;19(23):6519-23.