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Crenolanib

品牌：北京金优科技有限公司

货号	规格	包装/纯度	价格	货期	操作
JY-2025IT105mg	5mg	≥98%	¥1620.00 会员价请登录

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生物活性：	靶点：PDGFR;FLT3 通路：Angiogenesis; Protein Tyrosine Kinase/RTK 背景说明：Crenolanib是一种有效的,选择性PDGFRα/β抑制剂,也能有效抑制FLT3。生物活性：Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM， respectively.[1-3] In Vitro：Crenolanib has 25-fold more affinity for PDGFRA/B compared with KIT， and is approximately 135-fold more potent than STI571 for inhibiting the PDGFRA D842V mutation. The IC50 for crenolanib for a KIT exon 11 deletion mutant kinase is greater than 1，000 versus 8 nM for STI571. Crenolanib has low nanomolar potency against the V561D + D842V-mutant kinase that is similar to its potency against the isolated D842V mutation. Both STI571 and crenolanib potently inhibit the kinase activity of the fusion oncogene with IC50 values of 1 and 21 nM， respectively， and inhibits PDGFRA activation in this cell line with IC50 values of 93 and 26 nM， respectively[1]. HL60/VCR and K562/ABCB1 cells， overexpressing ABCB1， are 6.9- and 3.6-fold resistant to crenolanib， respectively， in relation to parental HL60 and K562 cells. PSC-833 fully reverses resistance to crenolanib in both HL60/VCR and K562/ABCB1 cells. Crenolanib (1 nM-10 μM) stimulates ABCB1 ATPase activity in a concentration-dependent manner. Crenolanib treatment does not increase the cell surface expression of ABCB1. Crenolanib inhibits [125I]-IAAP photocrosslinking of ABCB1 at high concentrations， with 50 % inhibition at 10 μM， but has little effect at lower concentrations， below 1 μM[2]. Crenolanib decreases NSCLC cell viability， induces apoptosis in NSCLC cells， and inhibits cell migration in NSCLC cells[3]. In Vivo：Crenolanib (10 mg/kg and 20 mg/kg) suppresses non-small-cell lung cancer tumor growth in vivo and induces tumor cell apoptosis， and the dosage of crenolanib applied is well tolerated by recipient mice[3]. 细胞实验：Viable cell numbers following drug treatment are measured using the WST-1 assay. Briefly， 1×103?cells are seeded in 100 μL complete medium per well in 96-well tissue culture plates and incubated with crenolanib (0-10?μM) at 37°C in 5% CO2 for 96 h. 10 μL WST-1 reagent is then added to each well， incubation is continued for two additional hours and the color developed is quantified according to the manufacturer’s instructions. Each experiment is performed in triplicate. IC50?concentrations are calculated by the least square fit of dose–response inhibition in a non-linear regression model using GraphPad Prism V software.[1-3] 动物实验：A549 cells are injected into the axillary regions of mice (2×106?cells/mouse). When the tumor volumes reached 70 mm3， the mice are randomLy allocated to the control group， low-dose crenolanib group (10 mg/kg)， or high-dose crenolanib group (20 mg/kg) (n=6 per group). The vehicle for crenolanib treatment consists of 10% 1-methyl-2-pyrrolidinone and 90% polyethylene glycol 300. The tumor size and mouse body weight are measured every other day for about 2 weeks. The tumor volume is calculated as follows: (mm3)=(width×width×length)/2. After treatment， the mice are euthanized using carbon dioxide， and the tumors are harvested and analyzed.[1-3] 数据来源文献：[1]. Heinrich MC， et al.Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with STI571-resistant gastrointestinal stromal tumors. Clin Cancer Res， 2012， Jun 27. [2]. Mathias TJ， et al. The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations. Invest New Drugs. 2015 Apr;33(2):300-9. [3]. Wang P， et al. Crenolanib， a PDGFR inhibitor， suppresses lung cancer cell proliferation and inhibits tumor growth in vivo. Onco Targets Ther. 2014 Sep 26;7:1761-8.
其它标识：	MDL：MFCD21609260 SMILES：NC1CCN(C2=CC=CC3=C2N=C(N4C5=CC=C(C=C5N=C4)OCC6(COC6)C)C=C3)CC1 InChIKey：DYNHJHQFHQTFTP-UHFFFAOYSA-N InChI：InChI=1S/C26H29N5O2/c1-26(14-32-15-26)16-33-20-6-7-22-21(13-20)28-17-31(22)24-8-5-18-3-2-4-23(25(18)29-24)30-11-9-19(27)10-12-30/h2-8,13,17,19H,9-12,14-16,27H2,1H3 PubChem CID：10366136
基本信息：	CAS：670220-88-9 英文名称：Crenolanib 别名：CP-868596;ARO 002 分子式：C₂₆H₂₉N₅O₂ 分子量：443.54 规格：2mg ; 5mg 溶解性：Soluble in DMSO ≥5mg/mL 纯度：≥98% 外观(性状)：Solid 储存条件：Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
靶点：	PDGFR;FLT3

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是一种有效的，选择性PDGFRα/β抑制剂，也能有效抑制FLT3。

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