Tirbanibulin-dihydrochloride-KX2-391-dihydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETirbanibulin dihydrochlorideCat. No.: HY-10340ACAS No.: 1038395-65-1Synonyms: KX2-391 (dihydrochloride); KX-01 (dihydrochloride)分式: CHClNO分量: 504.45作靶點(diǎn): Src; Microtubule/Tubulin作通路: Protein Tyrosine Kinase/RTK; Cell Cycle/DNA Da

2、mage;Cytoskeleton儲(chǔ)存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 33.33 mg/mL (66.07 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.9824 mL 9.9118 mL 19.8236 mL5 mM 0.3965 mL 1.9824 mL 3.9647 mL10 mM 0.1982 mL

3、 0.9912 mL 1.9824 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)先配制澄的儲(chǔ)備液，再依次添加助溶劑(為保證實(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: 2.5 mg/mL (4.96 mM); Clear solution2. 請(qǐng)依序添加每

4、種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.96 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (4.96 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)Sr

5、c 的抑制劑，在腫瘤細(xì)胞中，GI50 值為 9-60nM。IC50 & Target GI50: 9 nM (Src HuH7), 13 nM (Src PLC/PRF/5), 26 nM (Src Hep3B), 60 nM (Src HepG2)體外研究 Tirbanibulin (KX2-391) is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steepdose-response curves against Huh7 (GI50=9 nM), PLC/PRF/5 (GI50=

6、13 nM), Hep3B (GI50=26 nM), andHepG2 (GI50=60 nM), four hepatic cell cancer (HCC) cell lines 1. Tirbanibulin (KX2-391) is found to inhibitcertain leukemia cells that are resistant to current commercially available drugs, such as those derived fromchronic leukemia cells with the T3151 mutation. Tirba

7、nibulin (KX2-391) is evaluated in engineered Src drivencell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI50 with 23 nM and 39 nM,respectively 2.體內(nèi)研究 Orally administered Tirbanibulin (KX2-391) is shown to inhibit primary tumor growth and to suppressmetastasis, in pre-clinic

8、al animal models of cancer 2.PROTOCOLCell Assay 1 Liver cell lines including Huh7, PLC/PRF/5, Hep3B, and HepG2 are routinely cultured and maintained inbasal medium containing 2% fetal bovine serum (FBS) at 37C and 5% CO2. Cells are seeded at4.0103/190 L and 8.0103/190 L per well of 96-well plate in

9、basal medium containing 1.5% FBS. Theseare cultured overnight at 37C and 5% CO2 prior to the addition of Tirbanibulin (KX2-391), at concentrationsranging from 6,564 to 0.012 nM in triplicates. Treated cells are incubated for 3 days. Ten Ls of 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bro

10、mide (MTT) solution (5 mg/mL) is then added to each wellon day 3 and cells incubated for 4 hours. The formazan product is dissolved with 10% SDS in dilute HCl.Optical density at 570 nm is measured. For comparison of activity and potency, parallel experiments areperformed using Tirbanibulin (KX2-391)

11、. Growth inhibition curves, 50% inhibition concentration (GI50), and80% inhibition concentration (GI80) are determined using GraphPad Prism 5 statistical software. Data arenormalized to represent percentage of maximum response as well as reported in optical density atwavelength of 570 nm (OD570) sig

12、nal format.MCE has not independently confirmed the accuracy of these methods. They are for reference only. Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. Harvard Medical School LINCS LIBRARYSee more customer validations on HYPERLINK / www.MedChemE2/3 Master of Small Molecules 您邊的抑制劑師www.MedChem

13、EREFERENCES1. Lau GM, et al. Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma invitro. Dig Dis Sci, 2009, 54(7), 1465-1474.2. Fallah-Tafti A, et al. Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities. Eur JMed Chem, 2011, 46(10), 4853-4858.Mce