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

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 308 In-stock
Solution
10 mM * 1 mL in DMSO USD 308 In-stock
Solid
5 mg USD 280 In-stock
10 mg USD 450 In-stock
25 mg USD 790 In-stock
50 mg USD 1100 In-stock
100 mg USD 1500 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

ARN-21934 Related Antibodies

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Topoisomerase Topo I Topo II

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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

 

Cellular Effect
Cell Line Type Value Description References
A-375 IC50
12.6 μM
Compound: 14; ARN-21934
Antiproliferation activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferation activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33079544]
A549 IC50
17.1 μM
Compound: 14; ARN-21934
Antiproliferation activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferation activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33079544]
DU-145 IC50
11.5 μM
Compound: 14; ARN-21934
Antiproliferation activity against human DU145 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferation activity against human DU145 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33079544]
G-361 IC50
8.1 μM
Compound: 14; ARN-21934
Antiproliferation activity against human G361 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferation activity against human G361 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33079544]
HeLa IC50
38.2 μM
Compound: 14; ARN-21934
Antiproliferation activity against human Hela cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferation activity against human Hela cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33079544]
MCF7 IC50
15.8 μM
Compound: 14; ARN-21934
Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33079544]
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].

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

ARN-21934 Related Antibodies
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]

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

360.46

Formula

C21H24N6
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7742 mL 13.8712 mL 27.7423 mL 69.3558 mL
5 mM 0.5548 mL 2.7742 mL 5.5485 mL 13.8712 mL
10 mM 0.2774 mL 1.3871 mL 2.7742 mL 6.9356 mL
15 mM 0.1849 mL 0.9247 mL 1.8495 mL 4.6237 mL
20 mM 0.1387 mL 0.6936 mL 1.3871 mL 3.4678 mL
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ARN-21934 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ARN-219342230854-93-8ARN21934ARN 21934Topoisomeraseanticancertopoisomerase IIαDNA relaxationInhibitorinhibitorinhibit

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