INCB054329 _Epigenetic Reader Domain 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEINCB054329Cat. No.: HY-112504CAS No.: 1628607-64-6分式: CHNO分量: 348.36作靶點(diǎn): Epigenetic Reader Domain作通路: Epigenetics儲存式: 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 : 100 mg/mL (287.06 mM)* means

2、 soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.8706 mL 14.3530 mL 28.7059 mL5 mM 0.5741 mL 2.8706 mL 5.7412 mL10 mM 0.2871 mL 1.4353 mL 2.8706 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?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

3、現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，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. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.18 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.18 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master

4、of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (7.18 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 INCB054329種有效的 BET 抑制劑。IC50 & Target BET 1體外研究 INCB054329 is a bromodomain and extra-terminal motif (BET) inhibitor 1. INCB054329 inhibits binding ofBRD2, BRD3 and BRD4 to an acetylated histon

5、e H4 peptide with low nanomolar potency. In myeloma celllines, treatment with INCB054329 inhibits expression of c-MYC and induced HEXIM1. The majority ofmyeloma, AML, and lymphoma cell lines tested are growth inhibited by INCB054329 with potencies less than200 nM. Selectivity is seen when compared w

6、ith nontransformed cells as the potency for growth inhibition ofIL-2 stimulated T-cells from normal donors is greater than 1300 nM. Cell cycle analysis reveals treatment-induced G1 arrest. Furthermore in both AML and lymphoma cell lines, INCB054329 induces apoptosisconsistent with increased expressi

7、on of pro-apoptotic regulators 2.體內(nèi)研究 Oral administration of INCB054329 inhibits tumor growth in several models of hematologic cancers. In theMM1.S multiple myeloma xenograft model, inhibition of tumor growth is correlated with reduction of c-MYClevels. PK-PD analysis shows c-MYC suppression is asso

8、ciated with an IC50 value of less than 100 nM invivo 2.REFERENCES1. Prez-Salvia M, et al. Bromodomain inhibitors and cancer therapy: From structures to applications. Epigenetics. 2017 May 4;12(5):323-339.2. Phillip CC Liu, et al. Abstract 3523: Discovery of a novel BET inhibitor INCB054329.McePdfHeightCaution: Product has not been fully validated for medical applications