Cat. No.: HY-16228

Genz-644282

Name: Genz-644282
Brand: MedChemExpress
SKU: HY-16228
Price: 50.00 USD
Availability: InStock
Rating: 5 (2 reviews)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Genz-644282 is a non-camptothecin topoisomerase I inhibitor, used for cancer research.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté : 99.13%
CAS No.: 529488-28-6
Formule: C₂₂H₂₁N₃O₅
Masse moléculaire:407.42

Stockage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Genz-644282 Chemical Structure

CAS No.: 529488-28-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Genz-644282 is a non-camptothecin topoisomerase I inhibitor, used for cancer research.

IC₅₀ & Target

^[1]

Topoisomerase I

Voir tous les produits spécifiques à Isoform Topoisomerase :

Cellular Effect

Cell Line	Type	Value	Description	References
KB 3-1	IC₅₀	0.022 μM Compound: 6a	Inhibitory concentration against KB/V-1 cells overexpress MDR1 Inhibitory concentration against KB/V-1 cells overexpress MDR1	[PMID: 15689163]
KB 3-1	IC₅₀	0.0004 μM Compound: 6a	Inhibitory concentration against KB3-1 cell line was determined Inhibitory concentration against KB3-1 cell line was determined	[PMID: 15689163]
KB 3-1	IC₅₀	0.4 nM Compound: 6a	Inhibitory concentration against KB3-1 cell line was determined Inhibitory concentration against KB3-1 cell line was determined	[PMID: 15689163]
P388	IC₅₀	0.07 μM Compound: 6a	Inhibitory concentration against camptothecin-resistant variant of P388 cell line was determined Inhibitory concentration against camptothecin-resistant variant of P388 cell line was determined	[PMID: 15689163]
P388	IC₅₀	0.0003 μM Compound: 6a	Inhibitory concentration against P388 cell line in mouse leukemia was determine Inhibitory concentration against P388 cell line in mouse leukemia was determine	[PMID: 15689163]
P388	IC₅₀	0.3 nM Compound: 6a	Inhibitory concentration against P388 cell line in mouse leukemia was determine Inhibitory concentration against P388 cell line in mouse leukemia was determine	[PMID: 15689163]
RPMI 8402	IC₅₀	0.25 μM Compound: 6a	Cytotoxicity against camptothecin-resistant RPMI 8402 Cytotoxicity against camptothecin-resistant RPMI 8402	[PMID: 15689163]
RPMI 8402	IC₅₀	0.0003 μM Compound: 6a	Inhibitory concentration against lymphoblast RPMI 8402 cell line was determined Inhibitory concentration against lymphoblast RPMI 8402 cell line was determined	[PMID: 15689163]
RPMI 8402	IC₅₀	0.3 nM Compound: 6a	Inhibitory concentration against lymphoblast RPMI 8402 cell line was determined Inhibitory concentration against lymphoblast RPMI 8402 cell line was determined	[PMID: 15689163]

In Vitro

Genz-644282 is a topoisomerase I inhibitor. Genz-644282 shows potent activities against 29 human tumor cell lines with IC₅₀s ranging from 1.8 nM to 1.8 μM^[1]. Genz-644282 suppresses the PPTP cell lines, with IC₅₀s of 0.2-21.9 nM, and the mean IC₅₀ value is 1.2 nM^[2]. Genz-644282 is potent at trapping Top1-DNA covalent cleavage complexes. Genz-644282 (0.1 μM) induces γH2AX foci in human colon cancer HCT116 cells and breast cancer MCF7 cells. Genz-644282 is cytotoxic on the CPT-resistant human cancer cell lines^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .

In Vivo

Genz-644282 (1-4 mg/kg) is active when administered intravenously to the mice. Genz-644282 (2.7 mg/kg, i.v.) causes tumor growth delay (TGD) of 34 days in the human HCT-116 colon cancer xenograft, 27 days in the human HT-29 colon carcinoma xenograft and mice bearing the NCI-H460 human non-small cell lung carcinoma. Genz-644282 (2 mg/kg, i.v.) results in a TGD of 33 days in the human HCT-15 colon carcinoma xenograft, and 28 days in mice bearing LOX-IMVI melanoma. Moreover, Genz-644282 (1 mg/kg, i.v.) leads to 14 days of TGD in mice bearing the DLD-1 human colon carcinoma xenograft. Genz-644282 (1.7 mg/kg, i.v.) also produces a TGD of 23 days in mice bearing 786-O tumors and 33 days in NCI-H1299 human non-small cell lung carcinoma xenograft^[1]. Genz644282 at maximum tolerated dose (MTD, 4 mg/kg) results in maintained complete responses (MCR) in 6/6 evaluable solid tumor models. Genz644282 (2 mg/kg) induces CR or MCR in 3/3 tumor models and causes objective regressions in 7 of 17 (41%) models, but there are no objective responses at 1 mg/kg^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 529488-28-6
Appearance Solid
Masse moléculaire 407.42
Formule C₂₂H₂₁N₃O₅
Color White to light brown
SMILES

O=C1N(CCNC)C2=C(C=NC(C2=C3)=CC4=C3OCO4)C5=CC(OC)=C(OC)C=C15
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (2)

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Journal Impact Factor

Commun Biol

Mechanism of action of non-camptothecin inhibitor Genz-644282 in topoisomerase I inhibition. [Abstract]

2022 Sep 16;5(1):982. PMID: 36114357
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471

Solvant et solubilité

In Vitro:

DMSO : 3.64 mg/mL (8.93 mM; ultrasonic and warming and heat to 75°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4545 mL

12.2723 mL

24.5447 mL

5 mM

0.4909 mL

2.4545 mL

4.9089 mL

10 mM

---

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2 mg/mL (4.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

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

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

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

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4545 mL	12.2723 mL	24.5447 mL	61.3617 mL
DMSO	5 mM	0.4909 mL	2.4545 mL	4.9089 mL	12.2723 mL

Bioz

Keywords

Genz-644282

2 Cited Publications

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Genz-644282

Publications Citing Use of MedChemExpress (MCE) Genz-644282

Voir tous les produits spécifiques à Isoform Topoisomerase