SEL120-34A-monohydrochloride - CDK 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESEL120-34A monohydrochlorideCat. No.: HY-111388A分式: CHBrClN分量: 450.6作靶點(diǎn): CDK作通路: Cell Cycle/DNA Damage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 : 13 mg/mL (28.85 mM; Need ultrasonic)Mas

2、s Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.2193 mL 11.0963 mL 22.1926 mL5 mM 0.4439 mL 2.2193 mL 4.4385 mL10 mM 0.2219 mL 1.1096 mL 2.2193 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

3、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: 1.3 mg/mL (2.89 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 1.3 mg/mL (2.89 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 1.3 mg/mL (2.89 mM); Clear solutio

4、n1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 SEL120-34A monohydrochloride種選擇性的，ATP-競(jìng)爭(zhēng)性的 CDK8 抑制劑，對(duì) CDK8/CycC 和CDK19/CycC 復(fù)合物的 IC50 值分別為 4.4 nM 和 10.4 nM，對(duì) CDK8 的 Kd 值為 3 nM。SEL120-34Amonohydrochloride 對(duì) CDK9 的作很弱，計(jì)算的 IC50 值為 1070 nM，對(duì) CDK1、2、4、6、5、7 等作。SEL120-34A monohydr

5、ochloride 能夠抑制 STAT1 S727 和 STAT5 S726 的磷酸化。具有抗腫瘤活性 1。IC50 & Target CDK8/CycC CDK19/CycC CDK9/cycT4.4 nM (IC50) 10.4 nM (IC50) 1070 nM (IC50)體外研究 SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activitiesof CDK8/CycC and CDK19/CycC complexes with IC50

6、s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but showsno obvious activity against CDK1, 2, 4, 6, 5, 7 1.SEL120-34A (1.6 nM-5 M) inhibits the growth of STAT5 S726 positive KG-1 AML cells, but is not cyto

7、toxicto S726 negative MOLM13 AML cells 1.SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726, decreases IRF9and STAT1 mRNA expression and mitogen-induced IER expression 1.體內(nèi)研究 SEL120-34A monohydrochloride (30, 60 mg/kg, p.o. once every day) inhibits growth of AML tumor

8、s in adose-dependent manner in SCID mice after treatment for 17 days 1.REFERENCES1. Rzymski T, et al. SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 andSTAT5 transactivation domains. Oncotarget. 2017 May 16;8(20):33779-33795.McePdfHeightCaution: Product has not been fully validated for medical applications.