Shopping Cart
  • Remove All
  • TargetMol
    Your shopping cart is currently empty

Genz-644282

🥰Excellent
Catalog No. T7187Cas No. 529488-28-6
Alias Genz644282

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

Genz-644282

Genz-644282

🥰Excellent
Purity: 97.49%
Catalog No. T7187Alias Genz644282Cas No. 529488-28-6
Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment.
Pack SizePriceAvailabilityQuantity
1 mg38 €In Stock
2 mg51 €In Stock
5 mg76 €In Stock
10 mg122 €In Stock
25 mg207 €In Stock
50 mg311 €In Stock
100 mg471 €In Stock
1 mL x 10 mM (in DMSO)84 €In Stock
Bulk & Custom
Add to Cart
Questions
View More

Related Compound Libraries of "Genz-644282"

Select Batch
Purity:97.49%
Contact us for more batch information
Resource Download
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Product Introduction

Bioactivity
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].
AliasGenz644282
Chemical Properties
Molecular Weight407.42
FormulaC22H21N3O5
Cas No.529488-28-6
SmilesCNCCn1c2c3cc4OCOc4cc3ncc2c2cc(OC)c(OC)cc2c1=O
Relative Density.1.344 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 5 mg/mL (12.27 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4545 mL12.2723 mL24.5447 mL122.7235 mL
5 mM0.4909 mL2.4545 mL4.9089 mL24.5447 mL
10 mM0.2454 mL1.2272 mL2.4545 mL12.2723 mL

Calculator

  • Molarity Calculator
  • Dilution Calculator
  • Reconstitution Calculator
  • Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
%Tween 80
%ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

Related Tags: buy Genz-644282 | purchase Genz-644282 | Genz-644282 cost | order Genz-644282 | Genz-644282 chemical structure | Genz-644282 in vivo | Genz-644282 in vitro | Genz-644282 formula | Genz-644282 molecular weight