Lirametostat | CPI-1205 | CAS#1621862-70-1 | EZH2 inhibitor

Lirametostat
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206532

CAS#: 1621862-70-1

Description: Lirametostat, also known as CPI-1205 is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2. Upon oral administration, CPI-1205 selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 on lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased proliferation of EZH2-expressing cancer cells.

Chemical Structure

Lirametostat

CAS# 1621862-70-1

Instruction

Theoretical Analysis

MedKoo Cat#: 206532
Name: Lirametostat
CAS#: 1621862-70-1
Chemical Formula: C27H33F3N4O3
Exact Mass: 518.25
Molecular Weight: 518.581
Elemental Analysis: C, 62.54; H, 6.41; F, 10.99; N, 10.80; O, 9.26

Price and Availability

Size	Price	Availability
10mg	USD 450	2 Weeks
25mg	USD 750	2 Weeks
50mg	USD 1350	2 Weeks
100mg	USD 2250	2 Weeks
200mg	USD 3950	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: CPI-1205; CPI 1205; CPI1205; Lirametostat;

IUPAC/Chemical Name: (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide

InChi Key: HPODOLXTMDHLLC-QGZVFWFLSA-N

InChi Code: InChI=1S/C27H33F3N4O3/c1-16-13-23(37-4)21(25(35)32-16)14-31-26(36)24-18(3)34(22-8-6-5-7-20(22)24)17(2)19-9-11-33(12-10-19)15-27(28,29)30/h5-8,13,17,19H,9-12,14-15H2,1-4H3,(H,31,36)(H,32,35)/t17-/m1/s1

SMILES Code: C[C@@H](N1C2=C(C(C(NCC3=C(C=C(NC3=O)C)OC)=O)=C1C)C=CC=C2)C4CCN(CC(F)(F)F)CC4

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, not in water

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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 518.58 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.

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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1: Vaswani RG, Gehling VS, Dakin LA, Cook A, Nasveschuk CG, Duplessis M, Iyer P,
Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Cantone N, Cummings RT,
Normant E, Bellon SF, Albrecht BK, Harmange JP, Trojer P, Audia JE, Zhang Y,
Justin N, Chen S, Wilson J, Gamblin S. Identification of
(R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1
-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205),
a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for
Phase I Clinical Trials for B-Cell Lymphomas. J Med Chem. 2016 Oct 14. PubMed
PMID: 27739677.

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