SM-16 - TGF-β Receptor 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESM 16Cat. No.: HY-111482CAS No.: 614749-78-9分式: CHNO分量: 430.5作靶點(diǎn): TGF- Receptor作通路: TGF-beta/Smad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 : 65 mg/mL (150.99 mM; Need ultrasonic)Mass So

2、lvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.3229 mL 11.6144 mL 23.2288 mL5 mM 0.4646 mL 2.3229 mL 4.6458 mL10 mM 0.2323 mL 1.1614 mL 2.3229 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

3、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: 2.58 mg/mL (5.99 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.58 mg/mL (5.99 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.58 mg/mL (5.99 mM); Clear solution

4、1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 SM 16是ALK5/ALK4 激酶抑制劑，Ki 值分別為10 和 1.5 nM。IC50 & Target Ki: ALK5 (10 nM), ALK4 (1.5 nM) 1體外研究 SM 16 inhibits TGF-induced plasminogen activator inhibitor-luciferase activity (IC50=64 nM) and TGF- oractivin-induced Smad2 phosphoryl

5、ation at concentrations between 100 and 620 nM. SM 16 is tested against60 related and unrelated kinases and shows moderate off-target activity only against Raf (IC50=1 M) andp38/SAPKa (IC50=0.8 M). SM 16 exhibits no inhibitory activity against ALK family members ALK1 andALK6 1.體內(nèi)研究 SM 16 penetrates

6、tumor cells in vivo, suppressing tumor phosphorylated Smad2/3 levels for at least 3 hfollowing treatment of tumor-bearing mice with a single i.p. bolus of 20 mg/kg SM 16. The growth ofestablished AB12 tumors is significantly inhibited by 5 mg/kg/d SM 16 (P 1.PROTOCOLAnimal Mice 1Administration 1 BAL

7、B/c mice are injected on the right flank with 1106 AB12 tumor cells. Mice are randomly divided into twogroups and one group is implanted with minipumps loaded with 20% Captisol (control) on the left flank andthe other group is implanted with minipumps loaded with 20 mg/mL SM 16. Tumor recurrence is

8、defined asthe first day when a tumor is unambiguously visible or palpable. Plasma is obtained under anesthesia andanalyzed for SM 16 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Suzuki E, et al. A novel small-molecule inhibitor of tran

9、sforming growth factor beta type I receptor kinase (SM16) inhibits murinemesothelioma tumor growth in vivo and prevents tumor recurrence after surgical resection. Cancer Res. 2007 Mar 1;67(5):2351-9.2. Fu K, et al. SM16, an orally active TGF-beta type I receptor inhibitor prevents myofibroblast indu

10、ction and vascular fibrosis in the ratcarotid injury model. Arterioscler Thromb Vasc Biol. 2008 Apr;28(4):665-71.3. Engebretsen KV, et al. Attenuated development of cardiac fibrosis in left ventricular pressure overload by SM16, an orally active inhibitorof ALK5. J Mol Cell Cardiol. 2014 Nov;76:148-57.McePdfHeightCaution: Product has not been fully vali