>>Signaling Pathways>> Stem Cell>>EPZ004777 (formate)

EPZ004777 (formate)

Catalog No.GC48980

A potent inhibitor of DOT1L

Products are for research use only. Not for human use. We do not sell to patients.

EPZ004777 (formate) Chemical Structure

Cas No.: N/A

Size 가격 재고 수량
500 µg
US$43.00
재고 있음
1 mg
US$77.00
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5 mg
US$308.00
재고 있음
10 mg
US$403.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

EPZ004777 is a potent inhibitor of DOT1L (IC50 = 400 pM) that selectively kills mixed lineage leukemia (MLL) cells in vitro and prolongs survival in an MLL xenograft mouse model.1,2,3,4 It displays >1,000-fold selectivity for DOT1L relative to a panel of histone methyltransferases.1 DOT1L inhibition by EPZ004777 has also been shown to accelerate the reprogramming of somatic cells into induced pluripotent stem cells.5

1.Daigle, S.R., Olhava, E.J., Therkelsen, C.A., et al.Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitorCancer Cell.20(1)53-65(2011) 2.Chen, L., Deshpande, A.J., Banka, D., et al.Abrogation of MLL-AF10 and CALM-AF10-mediated transformation through genetic inactivation or pharmacological inhibition of the H3K79 methyltransferase Dot1lLeukemia27(4)813-822(2013) 3.Deshpande, A.J., Chen, L., Fazio, M., et al.Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1lBlood121(13)2533-2541(2013) 4.Yu, W., Chory, E.J., Wernimont, A.K., et al.Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitorsNat. Commun.31288(2012) 5.Ye, J., Ge, J., Zhang, X., et al.Pluripotent stem cells induced from mouse neural stem cells and small intestinal epithelial cells by small molecule compoundsCell Res.26(1)34-45(2016)

Chemical Properties

Cas No. N/A SDF
Canonical SMILES CC(C)(C)C1=CC=C(NC(NCCCN(C(C)C)C[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C=CC4=C3N=CN=C4N)O2)=O)C=C1.O=CO
Formula C28H41N7O4·CH2O2 M.Wt 585.7
Solubility DMF: 10 mg/ml,DMSO: 10 mg/ml,Ethanol: 10 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml Storage -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

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1 mg 5 mg 10 mg
1 mM 1.7074 mL 8.5368 mL 17.0736 mL
5 mM 0.3415 mL 1.7074 mL 3.4147 mL
10 mM 0.1707 mL 0.8537 mL 1.7074 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

리뷰

Review for EPZ004777 (formate)

Average Rating: 5 ★★★★★ (Based on Reviews and 4 reference(s) in Google Scholar.)

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