[1-[2-[5-(3-甲基氧雜環(huán)丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺

生物活性體外研究生物活性靶點(diǎn)體外研究 用途與合成方法 MSDS [1-[2-[5-(3-甲基氧雜環(huán)丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺價(jià)格(試劑級(jí)) 上下游產(chǎn)品信息

中文名稱	[1-[2-[5-(3-甲基氧雜環(huán)丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺
中文同義詞	PDGFRΑ/Β和FLT3抑制劑;1-[2-[5-[(3-甲基-3-氧雜環(huán)丁基)甲氧基]-1-苯并咪唑基]-8-喹啉基]-4-哌啶胺;[1-[2-[5-(3-甲基氧雜環(huán)丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺;CVC, TAK-652, TBR-652;化合物CRENOLANIB;CRENOLANIB中間體
英文名稱	Crenolanib
英文同義詞	Crenolanib, >=98%;Crenolanib;[1-[2-[5-(3-Methyloxetan-3-ylMethoxy)benziMidazol-1-yl]quinolin-8-yl]piperidin-4-yl]aMine;1-[2-[5-[(3-Methyl-3-oxetanyl)Methoxy]-1H-benziMidazol-1-yl]-8-quinolinyl]-4-piperidinaMine;ARO 002;CP 868596;Crenolanib (CP-868569);Crenolanib (CP-868596)
CAS號(hào)	670220-88-9
分子式	C26H29N5O2
分子量	443.54
EINECS號(hào)
相關(guān)類別	小分子抑制劑;信號(hào)轉(zhuǎn)導(dǎo)通路激酶抑制劑;小分子抑制劑，天然產(chǎn)物;細(xì)胞生物學(xué)試劑;蛋白酪氨酸激酶;抑制劑;標(biāo)準(zhǔn)品;Inhibitors;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Tyrosine Kinase Inhibitors
Mol文件	670220-88-9.mol
結(jié)構(gòu)式

[1-[2-[5-(3-甲基氧雜環(huán)丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺 性質(zhì)

[1-[2-[5-(3-甲基氧雜環(huán)丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺 用途與合成方法

生物活性

Crenolanib (CP-868596)是一種有效的，選擇性的PDGFRα/β抑制劑，K_d為2.1 nM/3.2 nM，也有效抑制FLT3，對(duì)D842V突變型而不是V561D突變型敏感，作用于PDGFR比作用于c-Kit， VEGFR-2， TIE-2， FGFR-2， EGFR， erbB2，和Src選擇性高100倍以上。

體外研究

Crenolanib is significantly more potent than imatinib in inhibiting the kinase activity of imatinib-resistant PDGFRα kinases (D842I, D842V, D842Y, D1842-843IM, and deletion I843). Crenolanib is 135-fold more otent than imatinib against D842V in the isogenic model system, with an IC50 of approximately 10 nM. Crenolanib inhibits the kinase activity of the fusion oncogene in EOL-1 cell line, which is derived from a patient with chronic eosinophilic leukemia and expresses the constitutively activated FIP1L1- PDGFRα fusion kinase, with IC50 = 21 nM. Crenolanib also inhibits the proliferation of EOL-1 cells with IC50 = 0.2 pM. Crenolanib inhibits the activation of V561D or D842V-mutant kinases expressed in BaF3 cells with IC50 with 85 nM or 272 nM, respectively. Crenolanib inhibits PDGFRα activation in H1703 non-small cell lung cancer cell line which has 24-fold amplification of the 4q12 region that contains the PDGFRα locus, with IC50 with 26 nM.  Crenolanib is an orally bioavailable, highly potent and selective PDGFR TKI. Crenolanib is a benzimidazole compound that has IC50s of 0.9 nM and 1.8 nM for PDGFRA and PDGFRB, respectively.

生物活性

Crenolanib (CP-868596, ARO 002)是一種有效的，選擇性PDGFRα/β抑制劑，在CHO細(xì)胞中Kd為2.1 nM/3.2 nM，也能有效抑制FLT3，對(duì)D842V突變型敏感對(duì)V561D突變型不敏感，作用于PDGFR比作用于c-Kit，VEGFR-2，TIE-2，F(xiàn)GFR-2，EGFR，erbB2，和Src的選擇性高100倍以上。Crenolanib可輔助誘導(dǎo)線粒體自噬。

靶點(diǎn)

體外研究

Crenolanib顯著比imatinib有效，能夠抑制對(duì)imatinib耐藥的PDGFRα激酶(D842I，D842V，D842Y，D1842-843IM，和缺失I843)活性。Crenolanib作用于同基因模型系統(tǒng)中D842V，比imatinib有效135倍，IC50大約為10 nM。Crenolanib抑制EOL-1細(xì)胞中融合致癌基因的激酶活性，其衍生自慢性噬酸細(xì)胞白血病患者，且表達(dá)持續(xù)活化的FIP1L1- PDGFRα融合激酶，IC50 = 21 nM。Crenolanib也會(huì)抑制EOL-1細(xì)胞的增殖，IC50 = 0.2 pM。Crenolanib抑制在BaF3細(xì)胞中表達(dá)的V561D或D842V突變激酶的活化，IC50分別為85 nM或272 nM。Crenolanib抑制H1703非小細(xì)胞肺癌細(xì)胞系中PDGFRα活化，其能夠使包含PDGFRα基因座的4q12區(qū)域擴(kuò)增24倍，IC50為26 nM。 Crenolanib是一種口服具有生物活性的，高度有效的，選擇性PDGFR TKI。Crenolanib是苯并咪唑化合物，對(duì)PDGFRA和PDGFRB的IC50s分別為0.9 nM和1.8 nM。

安全信息

MSDS信息

[1-[2-[5-(3-甲基氧雜環(huán)丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺 價(jià)格(試劑級(jí))

[1-[2-[5-(3-甲基氧雜環(huán)丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺 上下游產(chǎn)品信息