JQ-EZ-05
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MedKoo CAT#: 540228

CAS#: 1913252-04-6

Description: JQ-EZ-05, also known as JQEZ5 is a Potent and selective SAM-competitive EZH2 inhibitor (IC50 = 11 nM). JQ-EZ-05 selectively binds EZH2 over a panel of 22 methyltransferases.

Chemical Structure

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JQ-EZ-05
CAS# 1913252-04-6
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 540228
Name: JQ-EZ-05
CAS#: 1913252-04-6
Chemical Formula: C30H38N8O2
Exact Mass: 542.31
Molecular Weight: 542.688
Elemental Analysis: C, 66.40; H, 7.06; N, 20.65; O, 5.90

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 Weeks
100mg USD 750 2 Weeks
200mg USD 1350 2 Weeks
500mg USD 2850 2 Weeks
1g USD 3850 2 Weeks
2g USD 6450 2 Weeks
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Synonym: JQEZ5; JQEZ-5; JQEZ 5; JQ-EZ-05; JQ-EZ05; JQ-EZ 05;

IUPAC/Chemical Name: 1-isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide

InChi Key: LQTWDAYNGMMHLV-UHFFFAOYSA-N

InChi Code: InChI=1S/C30H38N8O2/c1-6-7-21-14-20(4)34-30(40)24(21)17-32-29(39)23-15-26(35-28-25(23)18-33-38(28)19(2)3)22-8-9-27(31-16-22)37-12-10-36(5)11-13-37/h8-9,14-16,18-19H,6-7,10-13,17H2,1-5H3,(H,32,39)(H,34,40)

SMILES Code: CC(C)N1N=CC2=C(C=C(N=C12)C3=CC=C(N4CCN(CC4)C)N=C3)C(NCC5=C(CCC)C=C(C)NC5=O)=O

Appearance: Solid powder

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: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

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:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitive inhibition of polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM.
In vitro activity: JQEZ5 and UNC1999 inhibited colony formation of primary human CD34+ CML stem/progenitor cells (Fig. 2D–E and Supplementary Fig. 3E–F). Reference: Cancer Discov. 2016 Nov;6(11):1237-1247. https://pubmed.ncbi.nlm.nih.gov/27630126/
In vivo activity: Tumor-bearing mice were then treated with JQEZ5 for three weeks (75 mg/kg IP daily) and the tumor volume of the lungs was comparatively visualized by MRI. Animals treated with JQEZ5 exhibited rapid and pronounced tumor regression over the three week treatment course, as demonstrated by two-dimensional MRI and volumetric measurements (Figure 7C). Reference: Cancer Discov. 2016 Sep;6(9):1006-21. https://pubmed.ncbi.nlm.nih.gov/27312177/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 17.9 33.03

Preparing Stock Solutions

The following data is based on the product molecular weight 542.69 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: 1. Xie H, Peng C, Huang J, Li BE, Kim W, Smith EC, Fujiwara Y, Qi J, Cheloni G, Das PP, Nguyen M, Li S, Bradner JE, Orkin SH. Chronic Myelogenous Leukemia- Initiating Cells Require Polycomb Group Protein EZH2. Cancer Discov. 2016 Nov;6(11):1237-1247. doi: 10.1158/2159-8290.CD-15-1439. Epub 2016 Sep 14. PMID: 27630126; PMCID: PMC5096974. 2. Zhang H, Qi J, Reyes JM, Li L, Rao PK, Li F, Lin CY, Perry JA, Lawlor MA, Federation A, De Raedt T, Li YY, Liu Y, Duarte MA, Zhang Y, Herter-Sprie GS, Kikuchi E, Carretero J, Perou CM, Reibel JB, Paulk J, Bronson RT, Watanabe H, Brainson CF, Kim CF, Hammerman PS, Brown M, Cichowski K, Long H, Bradner JE, Wong KK. Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer. Cancer Discov. 2016 Sep;6(9):1006-21. doi: 10.1158/2159-8290.CD-16-0164. Epub 2016 Jun 16. PMID: 27312177; PMCID: PMC5010480.
In vitro protocol: 1. Xie H, Peng C, Huang J, Li BE, Kim W, Smith EC, Fujiwara Y, Qi J, Cheloni G, Das PP, Nguyen M, Li S, Bradner JE, Orkin SH. Chronic Myelogenous Leukemia- Initiating Cells Require Polycomb Group Protein EZH2. Cancer Discov. 2016 Nov;6(11):1237-1247. doi: 10.1158/2159-8290.CD-15-1439. Epub 2016 Sep 14. PMID: 27630126; PMCID: PMC5096974. 2. Zhang H, Qi J, Reyes JM, Li L, Rao PK, Li F, Lin CY, Perry JA, Lawlor MA, Federation A, De Raedt T, Li YY, Liu Y, Duarte MA, Zhang Y, Herter-Sprie GS, Kikuchi E, Carretero J, Perou CM, Reibel JB, Paulk J, Bronson RT, Watanabe H, Brainson CF, Kim CF, Hammerman PS, Brown M, Cichowski K, Long H, Bradner JE, Wong KK. Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer. Cancer Discov. 2016 Sep;6(9):1006-21. doi: 10.1158/2159-8290.CD-16-0164. Epub 2016 Jun 16. PMID: 27312177; PMCID: PMC5010480.
In vivo protocol: 1. Zhang H, Qi J, Reyes JM, Li L, Rao PK, Li F, Lin CY, Perry JA, Lawlor MA, Federation A, De Raedt T, Li YY, Liu Y, Duarte MA, Zhang Y, Herter-Sprie GS, Kikuchi E, Carretero J, Perou CM, Reibel JB, Paulk J, Bronson RT, Watanabe H, Brainson CF, Kim CF, Hammerman PS, Brown M, Cichowski K, Long H, Bradner JE, Wong KK. Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer. Cancer Discov. 2016 Sep;6(9):1006-21. doi: 10.1158/2159-8290.CD-16-0164. Epub 2016 Jun 16. PMID: 27312177; PMCID: PMC5010480.

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