الصفحة الرئيسية>>Signaling Pathways>> Chromatin/Epigenetics>> Histone Methyltransferase>>EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate)

EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate) (Synonyms: EPZ-011989 trifluoroacetate)

رقم الكتالوجGC34136

EPZ-011989 trifluoroacetate هو مثبط قوي وفعال عن طريق الفم Zeste Homolog 2 (EZH2) مع استقرار التمثيل الغذائي. يحتوي EPZ-011989 trifluoroacetate على تثبيط مثبط لـ EZH2 بقيمة Ki أقل من 3 نانومتر. يُظهر EPZ-011989 trifluoroacetate تثبيطًا قويًا لعلامة الميثيل ونشاط مضاد للورم. يمكن استخدام ثلاثي فلورو أسيتات EPZ-011989 في البحث عن أنواع مختلفة من السرطان.

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EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate) التركيب الكيميائي

Cas No.: 1598383-41-5

الحجم السعر المخزون الكميّة
5mg
103٫00
متوفر
10mg
180٫00
متوفر
50mg
630٫00
متوفر
100mg
873٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate)

EPZ011989 trifluoroacetate is a potent, selective orally bioavailable EZH2 inhibitor with Ki 3000-fold selectivity over other HMTase.IC50 value: 15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. EPZ011989 also exhibits metabolic stability. Furthermore, EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. This functional response translates to activity in a long-term proliferation assay where EPZ011989 demonstrates an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM. In vivo: The LCC parameter, when corrected for plasma protein-binding, predicts an efficacious plasma level in mouse for EPZ011989 of 158 ng/mL. The pharmacokinetics in SCID mice following oral administration of 125, 250, 500, and 1000 mg/kg indicated that the 1000 mg/kg dose provided coverage over the LCC for 24 h, while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.

[1]. Campbell JE, et al. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. ACS Med Chem Lett. 2015 Mar 4;6(5):491-495.

Chemical Properties of EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate)

Cas No. 1598383-41-5 SDF
المرادفات EPZ-011989 trifluoroacetate
Canonical SMILES O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C#CCN3CCOCC3)=CC(N(CC)[C@H]4CC[C@H](N(CCOC)C)CC4)=C2C.O=C(O)C(F)(F)F
Formula C37H52F3N5O6 M.Wt 719.83
الذوبان DMSO : ≥ 34 mg/mL (47.23 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate)

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.3892 mL 6.9461 mL 13.8922 mL
5 mM 0.2778 mL 1.3892 mL 2.7784 mL
10 mM 0.1389 mL 0.6946 mL 1.3892 mL
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In vivo Formulation Calculator (Clear solution) of EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Average Rating: 5 ★★★★★ (Based on Reviews and 9 reference(s) in Google Scholar.)

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