Umbralisib-TGR-1202-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEUmbralisibCat. No.: HY-12279CAS No.: 1532533-67-7Synonyms: TGR-1202; RP5264分式: CHFNO分量: 571.55作靶點(diǎn): PI3K作通路: PI3K/Akt/mTOR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 : 20 mg/mL (34.99 mM;

2、Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.7496 mL 8.7481 mL 17.4963 mL5 mM 0.3499 mL 1.7496 mL 3.4993 mL10 mM 0.1750 mL 0.8748 mL 1.7496 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

3、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 90% corn oilSolubility: 2 mg/mL (3.50 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 Umbralisib (TGR-1202)是PI3K 抑制劑，IC50 和 EC50 值分別為 22.2 nM 和 24.3 nM；Umbralisib (TGR-1202) 同時(shí)可抑制 CK1，EC50 值為 6.0

4、M。IC50 & Target PI3K22.2 nM (IC50)體外研究 Umbralisib (RP5264) causes a half-maximal inhibition of human whole blood CD19 cell proliferation between100-300 nM 1. In human lymphoma and leukemia cell lines, Umbralisib (RP5264; 10 nM-100 M) inhibitsphosphorylated AKT at Ser473 in a concentration-dependent

5、manner. Umbralisib and PR-171 synergisticallykill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. Umbralisib and PR-171 in combinationsynergistically and selectively silence the c-Myc and E2F transcription programs. Umbralisib (15-50 M)potently represses the expression of c-Myc in

6、 the DLBCL cell line LY7, and is uniquely characterized withstructural features suitable for targeting CK1 in lymphoma cells 2.體內(nèi)研究 In a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice usingthe MOLT-4 cell line, Umbralisib (RP5264; 150 mg/kg, daily p.o.)

7、significantly shrinks the tumors by day 25 2.REFERENCES1. Swaroop Vakkalankaa, et al. Inhibition of PI3K kinase by a selective, small molecule inhibitor suppresses B-cell proliferation andleukemic cell growth.2. Deng C, et al. Silencing c-Myc translation as a therapeutic strategy through targeting PI3K and CK1 in hematological malignancies.Blood. 2017 Jan 5;129(1):88-99McePdfHeightCaution: Product has not been fully validated for medical applications.For resear