EPZ-719
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MedKoo CAT#: 408194

CAS#: 2697176-16-0 (free base)

Description: EPZ-719 is a novel and potent SETD2 inhibitor ( IC50 = 0.005 μM) with a high selectivity over other histone methyltransferases. SET domain-containing protein 2 (SETD2), a histone methyltransferase, has been identified as a target of interest in certain hematological malignancies, including multiple myeloma.

Chemical Structure

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EPZ-719
CAS# 2697176-16-0 (free base)
Instruction

Theoretical Analysis

MedKoo Cat#: 408194
Name: EPZ-719
CAS#: 2697176-16-0 (free base)
Chemical Formula: C22H31FN4O3S
Exact Mass: 450.21
Molecular Weight: 450.573
Elemental Analysis: C, 58.65; H, 6.94; F, 4.22; N, 12.43; O, 10.65; S, 7.12

Price and Availability

Size Price Availability Quantity
5mg USD 1150 2 Weeks
10mg USD 2150 2 Weeks
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Related CAS #: EPZ-719 HCl   2697176-16-0 (free base)   411757-44-1 (rel-)   EPZ-719 mesylate,  

Synonym: EPZ-719; EPZ 719; EPZ719;

IUPAC/Chemical Name: 1H-Indole-2-carboxamide, 4-fluoro-7-methyl-N-[(1R,3S)-3-[(3S)-3-[methyl(methylsulfonyl)amino]-1-pyrrolidinyl]cyclohexyl]-

InChi Key: ZLVKIBLQXFILMA-IKGGRYGDSA-N

InChi Code: InChI=1S/C22H31FN4O3S/c1-14-7-8-19(23)18-12-20(25-21(14)18)22(28)24-15-5-4-6-16(11-15)27-10-9-17(13-27)26(2)31(3,29)30/h7-8,12,15-17,25H,4-6,9-11,13H2,1-3H3,(H,24,28)/t15-,16+,17+/m1/s1

SMILES Code: O=C(C(N1)=CC2=C1C(C)=CC=C2F)N[C@H]3C[C@@H](N4C[C@@H](N(C)S(=O)(C)=O)CC4)CCC3

Appearance: To be determined

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 450.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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Lampe JW, Alford JS, Boriak-Sjodin PA, Brach D, Cosmopoulos K, Duncan KW, Eckley ST, Foley MA, Harvey DM, Motwani V, Munchhof MJ, Raimondi A, Riera TV, Tang C, Thomenius MJ, Totman J, Farrow NA. Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies. ACS Med Chem Lett. 2021 Aug 24;12(10):1539-1545. doi: 10.1021/acsmedchemlett.1c00272. PMID: 34671445; PMCID: PMC8521618.