1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIbrutinib-biotinCat. No.: HY-100342CAS No.: 1599432-18-4分式: CHNOS分量: 1097.37作靶點(diǎn): Btk作通路: Protein Tyrosine Kinase/RTK儲(chǔ)存式: Pure form -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 : 50 mg/mL (45.56 mM; Ne

2、ed ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 0.9113 mL 4.5563 mL 9.1127 mL5 mM 0.1823 mL 0.9113 mL 1.8225 mL10 mM 0.0911 mL 0.4556 mL 0.9113 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)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(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；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存

3、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 (2.28 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (2.28 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (2.28 mM)

4、; Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Ibrutinib-biotin種由 Ibrutinib 通過(guò)長(zhǎng)鏈接頭連接到物素上組成的探針，具體可參考WO2014059368A1 中 Compound 1-5，抑制 BTK，IC50 值為 0.755-1.02 nM。IC50 & Target IC50: 0.755-1.02 nM (BTK), 1.71-2.29 nM (TEC), 3.66-4.27 nM (BLK), 4.42-5.57 nM (BMX),

5、5.99-6.92 nM(LCK), 33.8-36.3 nM (Src), 0.187-0.198 M (ITK),5.34-4.87 M (JAK3) 1體外研究 Ibrutinib-biotin (Compound 1-5) is a probe that consists of Ibrutinib linked to biotin via a long chain linker.Ibrutinib is a TEC family kinase inhibitor. The TEC kinase family is composed of five members, TEC, BTK(B

6、rutons Tyrosine Kinase), ITK (interleukin-2-inducible T-cell kinase)/EMT/TSK, BMX and TXK/RLK. TheTEC family kinases participate in phosphotyrosine- mediated and phospholipid-mediated signaling systems.Many TEC family proteins are abundantly expressed in hematopoietic tissues, and play important rol

7、es in thegrowth and differentiation processes of blood cells 1.PROTOCOLKinase Assay 1 In this study, assay formats are tested for sensitivity, specificity, range, and to determine most suitable antiBTK Antibody. An aliquot of DOHH2 cell lysate (1 mg/mL) is inhibited with 1 M Ibrutinib then labeled w

8、ithprobe (1 M). Negative controls: Untreated DOHH2 and Jurkat cell lysates (l mg/mL) are labeled with probe(1 M) and Untreated DOHH2 cell lysate. Standard Streptavidin plate (5-pack); Read Buffer T (50 mL),SULFO TAG Goat Anti-mouse (50 g); SULFO TAG Goat Anti-rabbit (50 g); SULFO TAG streptavidin (5

9、0ug); MSD Standard Plates; MSD Blocker A; Protease inhibitor cocktail; Positive Control lysates from BTKexpressing cell line (DOHH2); Negative Control lysates; Ibrutinib (PCI); probe compound 1-5 (biotinylatedprobe).MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Betty Y. CHANG, et al. Companion diagnostics for tec family kinase inhibitor therapy. WO 2014059368 A1.McePdfHeightCaution: Product has not been fully validated for