OSI-930
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.
OSI-930是一种新型有效的Flt1、激酶插入结构域受体(KDR)、CSF-1R、Lck、c-Raf和活化受体酪氨酸激酶Kit的抑制剂,IC50值分别为8、9、15、22、41和80 nM[1]。
在其存活高度依赖于Kit 信号的HMC-1细胞系中,OSI-930抑制细胞增殖,诱导细胞凋亡。反之,在正常培养条件下的COLO-205细胞系中,OSI-930不抑制细胞生长。[1]。
OSI-930可时间和浓度依赖地使P450 3A4失去活性。此外,OSI-930可减少P450 3A4的CO差光谱[2]。
参考文献:
[1] Garton AJ1, Crew AP, Franklin M, Cooke AR, Wynne GM, Castaldo L, Kahler J, Winski SL, Franks A, Brown EN, Bittner MA, Keily JF, Briner P, Hidden C, Srebernak MC, Pirrit C, O'Connor M, Chan A, Vulevic B,Henninger D, Hart K, Sennello R, Li AH, Zhang T, Richardson F, Emerson DL, Castelhano AL, Arnold LD,Gibson NW. OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Res. 2006 Jan 15;66(2):1015-24.
[2] Lin HL1, Zhang H, Medower C, Hollenberg PF, Johnson WW. Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug. Drug Metab Dispos. 2011 Feb;39(2):345-50.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 443.44 |
Cas No. | 728033-96-3 |
Formula | C22H16F3N3O2S |
Solubility | ≥22.15 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide |
SDF | Download SDF |
Canonical SMILES | C1=CC=C2C(=C1)C(=CC=N2)CNC3=C(SC=C3)C(=O)NC4=CC=C(C=C4)OC(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。 |
Description | OSI-930是一种有效的受体酪氨酸激酶抑制剂,对c-Kit、KDR、Flt、CSF-1R、c-Raf和Lck的IC50值分别为80 nM、9 nM、8 nM、15 nM、41 nM和22 nM。 | |||||
靶点 | c-Kit | KDR | Flt | CSF-1R | c-Raf | Lck |
IC50 | 80 nM | 9 nM | 8 nM | 15 nM | 41 nM | 22 nM |
质量控制和MSDS
- 批次: