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Genz-644282

Cat. No. M3784

Genz-644282 Structure
Size Price Availability Quantity
5mg USD 110 In stock
10mg USD 200 In stock
50mg USD 495 In stock
100mg USD 860 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Genz-644282 is a cytotoxic agent and shows activity in several human tumor cell lines. In vitro, Genz-644282 demonstrated potent cytotoxic activity with a median IC(50) of 1.2 nM (range 0.2-21.9 nM). 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. Genz-644282 was highly active within a narrow dose range (2-4 mg/kg), typical of other topoisomerase I poisons. Genz-644282 has superior or equal antitumor activity in the human tumor xenografts than the standard compound comparators.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 407.42
Formula C22H21N3O5
CAS Number 529488-28-6
Purity >99%
Solubility DMSO
Storage at -20°C
References

Molecular and cellular pharmacology of the novel noncamptothecin topoisomerase I inhibitor Genz-644282.
Sooryakumar D, et al. Mol Cancer Ther. 2011 Aug;10(8):1490-9. PMID: 21636699.

Testing of the topoisomerase 1 inhibitor Genz-644282 by the pediatric preclinical testing program.
Houghton PJ, et al. Pediatr Blood Cancer. 2012 Feb;58(2):200-9. PMID: 21548007.

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

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Genz-644282 supplier, Topoisomerase, inhibitors

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