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Genz-644282

Catalog No. T7187 CAS 529488-28-6

Synonyms: Genz644282

Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Genz-644282, CAS 529488-28-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
5 mg	In stock	$ 117.00
10 mg	In stock	$ 198.00
25 mg	In stock	$ 352.00
50 mg	In stock	$ 517.00
100 mg	In stock	$ 739.00
1 mL * 10 mM (in DMSO)	In stock	$ 129.00

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Purity: 97.49%

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Description	Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment.
In vitro	Human bone marrow CFU-GM was more sensitive to the Top1 inhibitors than was mouse bone marrow CFU-GM. The ratio of mouse to human IC(90) values was more than 10 for the camptothecins and less than 10 for Genz-644282, which had more potency as a cytotoxic agent toward human tumor cells in culture than the camptothecins in the colony-forming and 72-hour proliferation assays. Genz-644282 has superior or equal antitumor activity in the human tumor xenografts than the standard drug comparators[1].
In vivo	In vivo, Genz-644282 at its MTD (4 mg/kg) induced maintained complete responses (MCR) in 6/6 evaluable solid tumor models. At 2 mg/kg Genz-644282 induced CR or MCR in 3/3 tumor models relatively insensitive to topotecan, but there were no objective responses at 1 mg/kg. Further testing at 2 mg/kg showed that Genz-644282 induced objective regressions in 7 of 17 (41%) models. There was a significant correlation between predictive response scores based on Affymetrix U133Plus2 baseline tumor expression profiles and the observed in vivo responses to Genz-644282[2].
Cell Research	Colony-forming assays were conducted with mouse and human bone marrow and eight human tumor cell lines. In addition, 29 human tumor cell lines representing a range of histology and potential resistance mechanisms were assayed for sensitivity to Genz-644282 in a 72-hour exposure assay. The efficacy of Genz-644282 was compared with standard anticancer drugs (i.e., irinotecan, docetaxel, and dacarbazine) in human tumor xenografts of colon cancer, renal cell carcinoma, non-small cell lung cancer, and melanoma[1].
Animal Research	Genz-644282 was tested against the PPTP in vitro panel (0.1 nM to 1 μM), and in vivo using three times per week × 2 schedule repeated at day 21 at its maximum tolerated dose (MTD) of 4 mg/kg. Subsequently Genz-644282 was tested at 4, 3, 2, and 1 mg/kg in 3 models to assess the dose-response relationship. mRNA gene signatures predictive for Genz-644282 response in vitro were applied to select 15 tumor models that were evaluated prospectively[2].

Synonyms	Genz644282
Molecular Weight	407.42
Formula	C22H21N3O5
CAS No.	529488-28-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5 mg/mL (12.27 mM)

References and Literature

1. Kurtzberg L S , Roth S , Krumbholz R , et al. Genz-644282, a Novel Non-Camptothecin Topoisomerase I Inhibitor for Cancer Treatment[J]. Clinical Cancer Research, 2011, 17(9):2777-2787. 2. Houghton P J , Lock R , Carol H , et al. Testing of the Topoisomerase 1 Inhibitor Genz644282 by the Pediatric Preclinical Testing Program[J]. Pediatric Blood & Cancer, 2012, 58(2):200-209.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Clinical Compound Library Bioactive Compounds Library Max Bioactive Compound Library NO PAINS Compound Library DNA Damage & Repair Compound Library

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Keywords

Genz-644282 529488-28-6 DNA Damage/DNA Repair Topoisomerase Genz 644282 Inhibitor inhibit Genz644282 inhibitor

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