Ki20227
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.
Ki20227对c-Fms、干细胞因子受体(c-Kit)、血管内皮生长因子受体2(KDR)和血小板衍生生长因子受体B的IC50值分别为2、451、12和217 nmol/L。
巨噬细胞集落刺激因子(M-CSF)在单核吞噬细胞群发育中必不可少,并参与免疫应答。 Ki20227(N-{4-[(6,7-二甲氧基-4-喹啉基)-氧基]-2-甲氧基苯基}-N'-[1-(1,3-噻唑-2-基)乙基]脲)是M-CSF受体(c-Fms)酪氨酸激酶的高选择性抑制剂。
体外:Ki20227抑制c-Fms、KDR、c-Kit和血小板衍生生长因子受体B,但不抑制其它激酶,如表皮生长因子受体、Fms样酪氨酸激酶3或c-Src。Ki20227还抑制M-NFS-60细胞的M-CSF依赖性生长,但不影响A375人黑色素瘤细胞的M-CSF依赖性生长。此外,Ki20227呈剂量依赖性地抑制抗酒石酸酸性磷酸酶阳性破骨细胞样细胞的发育[1]。
体内:在裸大鼠中,依次给予转移性肿瘤细胞以及心内注射A375细胞以建立实验模型,口服给予Ki20227抑制破骨细胞样细胞的积累和骨的重吸收。此外,在卵巢切除(ovx)的大鼠中,Ki20227降低抗酒石酸酸性磷酸酶阳性破骨细胞样细胞在骨表面上的数量[1]。
临床试验:目前,Ki20227正处于临床前开发阶段和暂无可用临床数据。
参考文献:
[1] Ohno H, Kubo K, Murooka H, Kobayashi Y, Nishitoba T, Shibuya M, Yoneda T, Isoe T. A c-fms tyrosine kinase inhibitor, Ki20227, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model. Mol Cancer Ther. 2006;5(11):2634-43.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 480.55 |
Cas No. | 623142-96-1 |
Formula | C24H24N4O5S |
Synonyms | Ki 20227;Ki-20227 |
Solubility | ≥48.1 mg/mL in DMSO; insoluble in H2O; ≥8.6 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 1-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-methoxyphenyl]-3-[1-(1,3-thiazol-2-yl)ethyl]urea |
SDF | Download SDF |
Canonical SMILES | CC(C1=NC=CS1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)OC |
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 | Ki20227是c-Fms酪氨酸激酶的高选择性抑制剂,其IC50值为2 nM。 | |||||
靶点 | c-Fms | VEGFR-2 | PDGFRβ | c-Kit | ||
IC50 | 2 nM | 12 nM | 217 nM | 451 nM |
质量控制和MSDS
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