IVALTINOSTAT

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C24H33N3O4
Molecular Weight	427.5365
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

SMILES

CN(C)CCCNC(=O)C(\COC1=C2C=CC=CC2=CC=C1)=C\CCCCC(=O)NO

InChI

InChIKey=AUGCSOFQTDKPSO-RGVLZGJSSA-N

InChI=1S/C24H33N3O4/c1-27(2)17-9-16-25-24(29)20(11-4-3-5-15-23(28)26-30)18-31-22-14-8-12-19-10-6-7-13-21(19)22/h6-8,10-14,30H,3-5,9,15-18H2,1-2H3,(H,25,29)(H,26,28)/b20-11+

HIDE SMILES / InChI

Description

CG-200745 is a novel inhibitor of histone deacetylases (HDACs), initially developed by CrystalGenomics, Inc for treatment of various hematological and solid cancers. Combinations of CG-200745 with SN38 (the active form of irinotecan), or oxaliplatin were more effective than the agents alone when used to inhibit the growth of HCT116 cells. The protein expressions of acetyl-H3, p21, caspase-3, -8, and -9, PARP, and XIAP were affected in a time- and dose-dependent manner in HCT116 cells treated with the CG-200745 alone or combined CG-200745 and SN-38. In HCT116 xenografts, the HDACI CG-200745 in combination with irinotecan dramatically inhibited tumor growth without showing additive toxicity.

Originator

Approval Year

PubMed

Show entries

Title	Date	PubMed
Effects of the HDAC inhibitor CG2 in combination with irinotecan, 5-fluorouracil, or oxaliplatin on HCT116 colon cancer cells and xenografts.	2010 Dec	21042746

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Patents

Sample Use Guides

In Vivo Use Guide

mice 30 mg/kg, 5 days/week

Route of Administration: Oral

Show entries

Name

Type

Language

IVALTINOSTAT

Official Name

English

CG-200745

Preferred Name

English

CG 2 (HDAC INHIBITOR)

Code

English

Ivaltinostat [WHO-DD]

Common Name

English

CG-2

Code

English

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Classification Tree

Code System

Code

Designated

FDA ORPHAN DRUG

919022

Designated

FDA ORPHAN DRUG

760420

Designated

FDA ORPHAN DRUG

846121

Designated

FDA ORPHAN DRUG

793520

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Code System

Code

Type

Description

EPA CompTox

DTXSID801028069

PRIMARY

SMS_ID

300000010881

PRIMARY

PUBCHEM

16117309

PRIMARY

CAS

936221-33-9

PRIMARY

MANUFACTURER PRODUCT INFORMATION

CG-200745

PRIMARY

Description: CG200745 is a novel hydroxamate-based pan-histone deacetylase inhibitor (HDACI). Like other inhibitors, CG200745 has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. CG200745 inhibited deacetylation of histone H3 and tubulin as much as vorinostat and belinostat did. CG200745 also inhibited growth of prostate cancer cells, increased sub-G1 population, and activated caspase-9, -3 and -8 in LNCaP, DU145 and PC3 cells. These results indicate that CG200745 induces apoptosis. The preclinical results show that combination treatment with docetaxel and new HDACI, CG200745, potentiated anti-tumor effect in hormone-refractory prostate cancer (HRPC) cells via activation of apoptosis. (Last update: 5/30/2016).

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ACTIVE MOIETY


					4I8MLM7L2H

IVALTINOSTAT

SALT/SOLVATE (PARENT)


					QA3Y8EZG57

IVALTINOSTAT PHOSPHATE