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Cat. No.: HY-133566

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Antitumor agent-22

Antitumor agent-22 is an inhibitor of topoisomerase I and II. Antitumor agent-22 can serve as a ROS-responsive prodrug, in which the boronate ester unit undergoes cleavage under the high ROS tumor microenvironment to release the active parent core, thereby inhibiting Top1/Top2. Antitumor agent-22 induces apoptosis in HCT116 cells and triggers G2 phase cell cycle arrest. Antitumor agent-22 exhibits antitumor activity in HCT116 xenograft mouse models in vivo. Antitumor agent-22 can be used for colon cancer-related research.

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CAS No.: 2415259-07-1
화학식: C₃₃H₃₃BFN₃O₆
분자량:597.44

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Antitumor agent-22 Chemical Structure

CAS No.: 2415259-07-1

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

Topoisomerase I

Topoisomerase II

All Topoisomerase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC50	0.016 μM	Antiproliferative activity against human HCT116 cells assessed as viability reduction by CCK8 assay. Antiproliferative activity against human HCT116 cells assessed as viability reduction by CCK8 assay.	32292547
MCF7	IC50	0.033 μM	Antiproliferative activity against human MCF-7 cells assessed as viability reduction by CCK8 assay. Antiproliferative activity against human MCF-7 cells assessed as viability reduction by CCK8 assay.	32292547
A549	IC50	0.037 μM	Antiproliferative activity against human A549 cells assessed as viability reduction by CCK8 assay. Antiproliferative activity against human A549 cells assessed as viability reduction by CCK8 assay.	32292547

In Vitro

OthersAnti-cancerApoptosis

Others

Antitumor agent-22 (compound 13a) (27.9-500 μM (Top1); 25-200 μM (Top2)) acts as a cell-free dual Top1/Top2 inhibitor, inhibiting Top1 at 83.3 μM and Top2 at 50 μM^[1].
Antitumor agent-22 releases the parent compound in response to H₂O₂ in PBS, with a release rate of 11.6% at 0.05 mM H₂O₂^[1].
Antitumor agent-22 exhibits potent antiproliferative activity against HCT116 colon cancer cells with an IC₅₀ of 16 nM^[1].
Antitumor agent-22 undergoes intracellular ROS-triggered cleavage in HCT116 cells, first converting to 15a and then to 1a within 8-72 h^[1].

Anti-cancer

Apoptosis

Antitumor agent-22 (0.05-0.4 μM; 24-48 h) induces apoptosis and G2 phase cell cycle arrest in HCT116 cells^[1].

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

Apoptosis Analysis^[1]

Cell Line:

HCT116 cells
Concentration:

0.05, 0.2, 0.4 μM
Incubation Time:

48 h
Result:

Induced apoptosis in HCT116 cells.

Cell Cycle Analysis^[1]

Cell Line:

HCT116 cells
Concentration:

0.05, 0.2, 0.4 μM
Incubation Time:

24 h
Result:

Induced G2 phase cell cycle arrest in HCT116 cells.

In Vivo

Anti-cancer

Antitumor agent-22 (compound 13a) (10 mg/kg; i.p., once daily for 21 days) achieves 64.4% tumor growth inhibition in the HCT116 xenograft mouse model without causing significant body weight loss^[1].

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

Related Protocols :

Chemical Information

CAS No. 2415259-07-1
분자량 597.44
화학식 C₃₃H₃₃BFN₃O₆
SMILES

O=C(OCC1=CC=C(B2OC(C)(C(C)(C)O2)C)C=C1)OC3=CC4=C(NC5=C4CCN6C(C7=CC(F)=CC=C7N(C56)C)=O)C=C3
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Li X, et al. Natural Product Evodiamine with Borate Trigger Unit: Discovery of Potent Antitumor Agents against Colon Cancer. ACS medicinal chemistry letters. 2020 Apr 09;11(4):439-444. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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