GENZ-644282 - CAS 529488-28-6
Catalog number: 529488-28-6
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C24H22F3N3O7
Molecular Weight:
521.44
COA:
Inquire
Targets:
Topoisomerase
Description:
Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations.
Appearance:
white solid powder
Synonyms:
GENZ-644282; GENZ644282; GENZ 644282.
MSDS:
Inquire
InChIKey:
BAORCAMWLWRZQG-UHFFFAOYSA-N
InChI:
InChI=1S/C22H21N3O5/c1-23-4-5-25-21-14-8-19-20(30-11-29-19)9-16(14)24-10-15(21)12-6-17(27-2)18(28-3)7-13(12)22(25)26/h6-10,23H,4-5,11H2,1-3H3
Canonical SMILES:
CNCCN1C2=C(C=NC3=CC4=C(C=C32)OCO4)C5=CC(=C(C=C5C1=O)OC)OC
Current Developer:
Genzyme.
1.Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment.
Kurtzberg LS1, Roth S, Krumbholz R, Crawford J, Bormann C, Dunham S, Yao M, Rouleau C, Bagley RG, Yu XJ, Wang F, Schmid SM, Lavoie EJ, Teicher BA. Clin Cancer Res. 2011 May 1;17(9):2777-87. doi: 10.1158/1078-0432.CCR-10-0542. Epub 2011 Mar 17.
PURPOSE: Genz-644282 [8,9-dimethoxy-5-(2-N-methylaminoethyl)-2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-one] has emerged as a promising candidate for antitumor agents. This report describes the bone marrow colony-forming unit, granulocyte macrophage (CFU-GM) and tumor cell CFU activity of topoisomerase I (Top1) inhibitors, such as Genz-644282, topotecan, irinotecan/SN-38, and ARC-111, and examines their activity in several human tumor xenograft models.
2.Testing of the topoisomerase 1 inhibitor Genz-644282 by the pediatric preclinical testing program.
Houghton PJ1, Lock R, Carol H, Morton CL, Gorlick R, Anders Kolb E, Keir ST, Reynolds CP, Kang MH, Maris JM, Billups CA, Zhang MX, Madden SL, Teicher BA, Smith MA. Pediatr Blood Cancer. 2012 Feb;58(2):200-9. doi: 10.1002/pbc.23016. Epub 2011 May 5.
BACKGROUND: Genz-644282 is a novel non-camptothecin topoisomerase I poison that is in clinical development.
3.Molecular and cellular pharmacology of the novel noncamptothecin topoisomerase I inhibitor Genz-644282.
Sooryakumar D1, Dexheimer TS, Teicher BA, Pommier Y. Mol Cancer Ther. 2011 Aug;10(8):1490-9. doi: 10.1158/1535-7163.MCT-10-1043. Epub 2011 Jun 2.
Camptothecin derivatives are powerful anticancer drugs because of their ability to trap topoisomerase I (Top1)-DNA cleavage complexes. However, they exhibit clinical limitations due to the instability of their α-hydroxylactone six-membered E-ring structure. In addition, they exhibit bone marrow and intestinal toxicity, especially in adults, and are drug efflux substrates. Here, we report a novel Top1 inhibitor, Genz-644282. We show that Genz-644282 and its metabolites induce Top1 cleavage at similar, as well as unique genomic positions, compared with camptothecin. The compound also induces protein-linked DNA breaks and Top1-DNA cleavage complexes that persist longer after compound removal than camptothecin. Concentration-dependent and persistent γH2AX formation was readily observed in cells treated with Genz-644282, and was present in greater than 50% of the cell population following 24 hours compound exposure. The compound shows partial cross-resistance in cell lines resistant to camptothecin.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Topoisomerase Products


CP 117227
(CAS: 154531-78-9)

CP 117227, a dibenzocyclohepten derivative, has been found to be a Type II DNA topoisomerase inhibitor that was once developed in studies of anticancer.

CAS 174634-09-4 TAS-103

TAS-103
(CAS: 174634-09-4)

TAS-103, also known as BMS-247615, is a quinoline derivative that displays antitumor activity in murine and human tumor models. TAS-103 has been reported to be ...

CAS 95343-20-7 Pirarubicin Hydrochloride

Pirarubicin Hydrochloride
(CAS: 95343-20-7)

Pirarubicin Hydrochloride is an analogue of the anthracycline anti-neoplastic doxorubicin, which is an inhibitor of Topo II. It intercalates into DNA and intera...

CAS 161967-81-3 Grepafloxacin Hydrochloride

Grepafloxacin Hydrochloride
(CAS: 161967-81-3)

The hydrochloride salt form of Grepafloxacin, a fluoroquinolone derivative, has been found to be a Type II DNA topoisomerase inhibitor and was once studied as a...

CAS 186668-40-6 (±)-E-Homocamptothecin

(±)-E-Homocamptothecin
(CAS: 186668-40-6)

(±)-E-Homocamptothecin is a potent topoisomerase I (Topo 1) inhibitor.

CAS 529488-28-6 GENZ-644282

GENZ-644282
(CAS: 529488-28-6)

Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibi...

NSC 660028
(CAS: 153230-81-0)

NSC 660028, an arylamino etoposide analogue, has been found to be a DNA topoisomerase II inhibitor that was once studied due to its potential anticancer activit...

CAS 119914-60-2 Grepafloxacin

Grepafloxacin
(CAS: 119914-60-2)

Grepafloxacin is a quinoline antibacterial agent used to treat various bacterial infections.

Chemical Structure

CAS 529488-28-6 GENZ-644282

Quick Inquiry

Verification code

Featured Items