1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. ARN-21934

ARN-21934 

Cat. No.: HY-137466
Handling Instructions

ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research.

For research use only. We do not sell to patients.

ARN-21934 Chemical Structure

ARN-21934 Chemical Structure

CAS No. : 2230854-93-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research[1].

IC50 & Target[1]

topoisomerase II alpha

 

topoisomerase II beta

 

In Vitro

ARN-21934 display a different affinity for topoIIα and topoIIβ. ARN-21934 is more potent against the α isoform, the IC50 value for the inhibition of DNA relaxation by topoIIα is 2 μM, the value for inhibition of DNA relaxation by topoIIβ is 120 μM[1].
ARN-21934 exhibits a small panel of human cancer cell lines. It against melanoma (A375 and G-361), breast (MCF7), endometrial (HeLa), lung (A549), and androgen-independent prostate (DU145) cancer cells with IC50 values of 12.6 μM, 8.1 μM, 15.8 μM, 38.2 μM, 17.1 μM, and 11.5 μM, respectively[1].

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

In Vivo

ARN-21934 (intraperitoneal injection; 10 mg/kg; single dose) reaches a maximal plasma concentration of 0.68 μg/mL after 15 min. The half-life is 149 min in circulation, still being present in plasma 360 min after injection. The compound also exhibits good clearance values (0.116 L/(min kg)). Besides, ARN-21934 is able to reach the brain, with a maximum concentration of compound at 60 min, and is still present in the brain 360 min after injection[1]

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

Molecular Weight

360.46

Formula

C₂₁H₂₄N₆

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 8.33 mg/mL (23.11 mM; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7742 mL 13.8712 mL 27.7423 mL
5 mM 0.5548 mL 2.7742 mL 5.5485 mL
10 mM 0.2774 mL 1.3871 mL 2.7742 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

ARN-21934ARN21934ARN 21934Topoisomeraseanticancertopoisomerase IIαDNA relaxationInhibitorinhibitorinhibit

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