ARN-21934

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MedKoo CAT#: 463236

CAS#: unknown

Description: ARN-21934 is a Highly Selective for Human Topoisomerase II α over β. ARN-21934 showed IC50 = 2 μM for inhibition of DNA relaxation, as compared to an IC50 = 120 μM for the anticancer drug etoposide with excellent metabolic stability and solubility. This new compound also shows ~100-fold selectivity for topoIIα over topoβ, a broad antiproliferative activity toward cultured human cancer cells, a favorable in vivo pharmacokinetic profile, and the ability to penetrate the blood−brain barrier. Thus, ARN-21934 is a highly promising lead for the development of novel and potentially safer topoII-targeted anticancer drugs.

Chemical Structure

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ARN-21934
CAS# unknown
Instruction

Theoretical Analysis

MedKoo Cat#: 463236
Name: ARN-21934
CAS#: unknown
Chemical Formula: C21H24N6
Exact Mass: 360.21
Molecular Weight: 360.465
Elemental Analysis: C, 69.97; H, 6.71; N, 23.31

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: ARN-21934; ARN21934; ARN 21934;

IUPAC/Chemical Name: N4-(4-(dimethylamino)phenyl)-2-(pyridin-4-yl)-5,6,7,8-tetrahydroquinazoline-4,6-diamine

InChi Key: CKXSRLUXTFDZCF-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H24N6/c1-27(2)17-6-4-16(5-7-17)24-21-18-13-15(22)3-8-19(18)25-20(26-21)14-9-11-23-12-10-14/h4-7,9-12,15H,3,8,13,22H2,1-2H3,(H,24,25,26)

SMILES Code: NC1CC2=C(NC3=CC=C(N(C)C)C=C3)N=C(C4=CC=NC=C4)N=C2CC1

Appearance: 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

Shelf Life: >3 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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 360.47 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Ortega JA, Arencibia JM, Minniti E, Byl JAW, Franco-Ulloa S, Borgogno M, Genna V, Summa M, Bertozzi SM, Bertorelli R, Armirotti A, Minarini A, Sissi C, Osheroff N, De Vivo M. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. J Med Chem. 2020 Oct 20. doi: 10.1021/acs.jmedchem.0c00774. Epub ahead of print. PMID: 33079544.