貨號	規格	價格	上海	北京	武漢	南京
S80882-5mg	98.7%	￥340.00 S80882-5mg ￥340.00 現貨	9 9	-	-	-
S80882-10mg	98.7%	￥544.00 S80882-10mg ￥544.00 現貨	8 8	-	-	-
S80882-50mg	98.7%	￥1700.00 S80882-50mg ￥1700.00 現貨	2 2	-	-	-

產品介紹

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.

產品描述：

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.

靶點：

PDGFRα:2.1 nM (Kd);PDGFRβ:3.2 nM (Kd);FLT3:0.74 nM (Kd);FLT;PDGFR;Autophagy

體外研究：

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. 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. Crenolanib decreases NSCLC cell viability, induces apoptosis in NSCLC cells, and inhibits cell migration in NSCLC cells

體內研究：

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

參考文獻：

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.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.255 ml	11.273 ml	22.546 ml
5 mM	0.451 ml	2.255 ml	4.509 ml
10 mM	0.225 ml	1.127 ml	2.255 ml
50 mM	0.045 ml	0.225 ml	0.451 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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Crenolanib (CP-868596)