Tyrosine-kinase-IN-1 - VEGFR 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETyrosine kinase-IN-1Cat. No.: HY-100315CAS No.: 705946-27-6分式: CHFNO分量: 445.53作靶點(diǎn): VEGFR; PDGFR; FGFR作通路: Protein Tyrosine Kinase/RTK儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 62.5 mg/

2、mL (140.28 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.2445 mL 11.2226 mL 22.4452 mL5 mM 0.4489 mL 2.2445 mL 4.4890 mL10 mM 0.2245 mL 1.1223 mL 2.2445 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為

3、保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.67 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.67 mM); Clear solution1/2 Master of Small Mo

4、lecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Tyrosine kinase-IN-1是多靶點(diǎn)的酪氨酸激酶抑制劑，抑制 KDR，F(xiàn)lt-1，F(xiàn)GFR1 和 PDGFR 的 IC50 值分別為4，20，4，2 nM。IC50 & Target Flt-1 KDR PDGFR FGFR14 nM (IC50) 20 nM (IC50) 4 nM (IC50) 2 nM (IC50)體外研究 Tyrosine kinase-IN-1 is from reference (compound 8K) 1.體內(nèi)研究 Tyrosine kinase-IN

5、-1 shows a reasonable PK profile (AUC(0)=1.9, t1/2=4.6 h). It has a favorable oralbioavailability (F=63%) in rats 1.PROTOCOLKinase Assay 1 Kinase Inhibition Assays Kinase activities of KDR and PDGFR are measured as the percent of ATPconsumed following the kinase reaction using luciferaseluciferin-co

6、upled chemiluminescence. Kinasereactions are initiated by combining test compound (Tyrosine kinase-IN-1), ATP, kinases and substrates in a20 mL volume using 384-well microtiter plates. For KDR, the final reaction mixture contained 3 mM ATP, 1.6mM poly(Glu, Tyr) 4:1 and 1.5 nM KDR of residues D807-V1

7、356 with an N-terminal GST tag. For PDGFR,the final reaction mixture contained 2 mM ATP, 10 mM MBP and 14 nM PDGFR of residues Q551-L1089with an N-terminal GST tag. The reaction mixture is incubated at room temperature for 4 h (KDR) or 2 hPDGFR before a 20 mL aliquot of Kinase Glo is added and lumin

8、escence signal is measured using aVictor2 plate reader. Total ATP consumption is limited below 50% 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Moon K, et al. The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorganic & MedicinalChemistry Letters 22 (2012) 49794985McePdfHeightCaution: Product has not been fully validated for medical applicat