GENZ-644282
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MedKoo CAT#: 205471

CAS#: 529488-28-6 (free base)

Description: Genz-644282, also known as SAR402674, 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.


Chemical Structure

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GENZ-644282
CAS# 529488-28-6 (free base)

Theoretical Analysis

MedKoo Cat#: 205471
Name: GENZ-644282
CAS#: 529488-28-6 (free base)
Chemical Formula: C24H22F3N3O7
Exact Mass: 407.14812
Molecular Weight: 521.44
Elemental Analysis: C, 55.28; H, 4.25; F, 10.93; N, 8.06; O, 21.48

Price and Availability

Size Price Availability Quantity
25.0mg USD 150.0 Same day
50.0mg USD 250.0 Same day
100.0mg USD 450.0 Same day
200.0mg USD 850.0 Same day
500.0mg USD 1650.0 Same day
1.0g USD 2950.0 Same day
2.0g USD 5250.0 Same day
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Related CAS #: 529488-28-6 (free base)   1238632-19-3 (citrate)    

Synonym: GENZ644282; GENZ-644282; GENZ 644282; SAR402674; SAR 402674; SAR-402674.

IUPAC/Chemical Name: 2,3-dimethoxy-12-(2-(methylamino)ethyl)-[1,3]dioxolo[4',5':4,5]benzo[1,2-h]benzo[c][1,6]naphthyridin-13(12H)-one

InChi Key: BAORCAMWLWRZQG-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: O=C1N(CCNC)C2=C(C=NC3=CC(OCO4)=C4C=C32)C5=CC(OC)=C(OC)C=C15

Appearance: Yellow 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

Preparing Stock Solutions

The following data is based on the product molecular weight 521.44 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

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1: Sooryakumar D, Dexheimer TS, Teicher BA, Pommier Y. Molecular and cellular pharmacology of the novel noncamptothecin topoisomerase I inhibitor Genz-644282. Mol Cancer Ther. 2011 Aug;10(8):1490-9. Epub 2011 Jun 2. PubMed PMID: 21636699; PubMed Central PMCID: PMC3155218.

2: Houghton PJ, 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. Testing of the topoisomerase 1 inhibitor Genz-644282 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2011 May 5. doi: 10.1002/pbc.23016. [Epub ahead of print] PubMed PMID: 21548007; PubMed Central PMCID: PMC3154998.

3: Kurtzberg LS, 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. Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment. Clin Cancer Res. 2011 May 1;17(9):2777-87. Epub 2011 Mar 17. PubMed PMID: 21415217.