网站主页 >> CAS数据库列表 >> [1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺
[1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺
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- CAS号:
- 670220-88-9
- 英文名:
- Crenolanib
- 英文别名:
- 596;CS-72;CP-868;RO 002;ARO 002;CP868569;CP 868596;Crenolanib;Crenolanib, >=98%;CP868569/Crenolanib
- 中文名:
- [1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺
- 中文别名:
- CRENOLANIB中间体;化合物CRENOLANIB;PDGFRΑ/Β和FLT3抑制剂;CVC, TAK-652, TBR-652;1-[2-[5-[(3-甲基-3-氧杂环丁基)甲氧基]-1-苯并咪唑基]-8-喹啉基]-4-哌啶胺;[1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺
- CBNumber:
- CB02582957
- 分子式:
- C26H29N5O2
- 分子量:
- 443.54
- MOL File:
- 670220-88-9.mol
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[1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺化学性质
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沸点:
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676.6±65.0 °C(Predicted)
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密度:
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1.36
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储存条件:
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-20°
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溶解度:
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Soluble in DMSO (up to 15 mg/ml) or in Ethanol (up to 10 mg/ml).
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形态:
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solid
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酸度系数(pKa):
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9.84±0.20(Predicted)
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颜色:
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White
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稳定性:
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Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
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CAS 数据库:
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670220-88-9
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[1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺性质、用途与生产工艺
Crenolanib (CP-868596)是一种有效的，选择性的PDGFRα/β抑制剂，K
d为2.1 nM/3.2 nM，也有效抑制FLT3，对D842V突变型而不是V561D突变型敏感，作用于PDGFR比作用于c-Kit， VEGFR-2， TIE-2， FGFR-2， EGFR， erbB2，和Src选择性高100倍以上。
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.
Crenolanib (CP-868596, ARO 002)是一种有效的，选择性PDGFRα/β抑制剂，在CHO细胞中Kd为2.1 nM/3.2 nM，也能有效抑制FLT3，对D842V突变型敏感对V561D突变型不敏感，作用于PDGFR比作用于c-Kit，VEGFR-2，TIE-2，FGFR-2，EGFR，erbB2，和Src的选择性高100倍以上。Crenolanib可辅助诱导线粒体自噬。
| Target | Value |
FLT3
(CHO cells)
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0.74 nM(Kd)
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PDGFRα
(CHO cells)
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2.1 nM(Kd)
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PDGFRβ
(CHO cells)
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3.2 nM(Kd)
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Crenolanib显著比imatinib有效，能够抑制对imatinib耐药的PDGFRα激酶(D842I，D842V，D842Y，D1842-843IM，和缺失I843)活性。Crenolanib作用于同基因模型系统中D842V，比imatinib有效135倍，IC50大约为10 nM。Crenolanib抑制EOL-1细胞中融合致癌基因的激酶活性，其衍生自慢性噬酸细胞白血病患者，且表达持续活化的FIP1L1- PDGFRα融合激酶，IC50 = 21 nM。Crenolanib也会抑制EOL-1细胞的增殖，IC50 = 0.2 pM。Crenolanib抑制在BaF3细胞中表达的V561D或D842V突变激酶的活化，IC50分别为85 nM或272 nM。Crenolanib抑制H1703非小细胞肺癌细胞系中PDGFRα活化，其能够使包含PDGFRα基因座的4q12区域扩增24倍，IC50为26 nM。 Crenolanib是一种口服具有生物活性的，高度有效的，选择性PDGFR TKI。Crenolanib是苯并咪唑化合物，对PDGFRA和PDGFRB的IC50s分别为0.9 nM和1.8 nM。
[1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-13223 | Crenolanib | | 1 mg | 380元 |
| 2024/01/25 | HY-13223 | [1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺
Crenolanib | 670220-88-9 | 5mg | 900元 |
[1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺
生产厂家
670220-88-9, [1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺 相关搜索:
- Tyrosine Kinase Inhibitors
- Pharmaceuticals
- Intermediates & Fine Chemicals
- Heterocycles
- Aromatics
- Inhibitors
- 药靶配体
- 合成有机化合物配体
- 化工试剂
- 标准品
- 抑制剂
- 细胞生物学试剂
- 蛋白酪氨酸激酶
- 小分子抑制剂，天然产物
- 信号转导通路激酶抑制剂
- 小分子抑制剂
- CRENOLANIB中间体
- 化合物CRENOLANIB
- CVC, TAK-652, TBR-652
- PDGFRΑ/Β和FLT3抑制剂
- 1-[2-[5-[(3-甲基-3-氧杂环丁基)甲氧基]-1-苯并咪唑基]-8-喹啉基]-4-哌啶胺
- [1-[2-[5-(3-甲基氧杂环丁烷-3-基甲氧基)苯并咪唑-1-基]喹啉-8-基]哌啶-4-基]胺
- 670220-88-9
- RO 002
- Crenolanib USP/EP/BP
- 4-Piperidinamine, 1-[2-[5-[(3-methyl-3-oxetanyl)methoxy]-1H-benzimidazol-1-yl]-8-quinolinyl]-
- CRENOLANIB;CP-868596;CP 868596;ARO 002
- CP868569
- CP-868;596; CP-868596; ARO 002;CP868596
- CP-868
- 596
- CS-72
- 1-[2-[5-[(3-Methyl-3-oxetanyl)methoxy]-1-benzimidazolyl]-8-quinolyl]-4-piperidinamine
- 1-(2-(5-((3-Methyloxetan-3-yl)methoxy)-1H-benzo-[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-ami
- [1-[2-[5-(3-Methyloxetan-3-ylmethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-yl]amine Crenolanib ,ARO 002
- 1-(2-(5-((3-methyloxetan-3-yl)methoxy)-1H-benzo[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-amine
- cp-868596 crenolanib
- CP868569/Crenolanib
- Crenolanib (CP-868596)
- Crenolanib (CP-868569)
- CP 868596
- ARO 002
- 1-[2-[5-[(3-Methyl-3-oxetanyl)Methoxy]-1H-benziMidazol-1-yl]-8-quinolinyl]-4-piperidinaMine
- [1-[2-[5-(3-Methyloxetan-3-ylMethoxy)benziMidazol-1-yl]quinolin-8-yl]piperidin-4-yl]aMine
- Crenolanib
- Crenolanib, >=98%