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Cat. No.: HY-146080

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Antitumor agent-61

Antitumor agent-61 (Compound 9b), Irinotecan (Ir) derivative, is a potential antitumor agent. Antitumor agent-61 displays potent activity with IC₅₀s of 0.92, 1.39, 1.75, 2.20, 3.05 and 3.23 μM against five human cancer cells SK-OV-3, SK-OV-3/CDDP, U2OS, MCF-7, A549 and MG-63, respectively. Antitumor agent-61 induces SK-OV-3 cells apoptosis through mitochondrion pathways.

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

CAS No.: 2408917-12-2
Formula: C₅₄H₆₃FN₅O₁₀P
Molecular Weight:992.08

Storage:

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

Data Sheet (279 KB)

Antitumor agent-61 Chemical Structure

CAS No.: 2408917-12-2

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

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	3.05 μM Compound: 9b	Cytotoxicity against human A549 cells assessed as reduction in cell growth by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell growth by MTT assay	[PMID: 31972391]
MCF7	IC₅₀	2.2 μM Compound: 9b	Cytotoxicity against human MCF-7 cells assessed as reduction in cell growth by MTT assay Cytotoxicity against human MCF-7 cells assessed as reduction in cell growth by MTT assay	[PMID: 31972391]
MG-63	IC₅₀	3.23 μM Compound: 9b	Cytotoxicity against human MG-63 cells assessed as reduction in cell growth by MTT assay Cytotoxicity against human MG-63 cells assessed as reduction in cell growth by MTT assay	[PMID: 31972391]
SK-OV-3	IC₅₀	0.92 μM Compound: 9b	Cytotoxicity against human SK-OV-3 cells assessed as reduction in cell growth by MTT assay Cytotoxicity against human SK-OV-3 cells assessed as reduction in cell growth by MTT assay	[PMID: 31972391]
U2OS	IC₅₀	1.75 μM Compound: 9b	Cytotoxicity against human U2OS cells assessed as reduction in cell growth by MTT assay Cytotoxicity against human U2OS cells assessed as reduction in cell growth by MTT assay	[PMID: 31972391]

In Vitro

Antitumor agent-61 (compound 6b) shows anti-proliferation activity with IC₅₀ values of 3.05, 2.20, 3.23, 1.75, 0.92 and 1.39 μM for A549, MCF-7, MG-63, U2OS, SK-OV-3 and SK-OV-3/CDDP cells^[1].
Antitumor agent-61 (compound 6b) (50-150 μM) shows a certain inhibitory activity against Topo I at 150 μM^[1].
Antitumor agent-61 (compound 6b) (5-10 μM; 24 hours, SK-OV-3 cells) induces apoptosis through mitochondrial pathway. Decrease the MMP level and increase ROS level in a dose-dependent manner ^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

SK-OV-3 cells
Concentration:

5.0 and 10 μM
Incubation Time:

24 hours
Result:

Increased the percentage of apoptosis cells (including the early and late apoptosis) from 21.11% (5 μM) to 32.27% (10 μM), respectively and the apoptosis rate was significantly greater than that of Ir.

Cell Cycle Analysis^[1]

Cell Line:

SK-OV-3 cells
Concentration:

5.0 and 10 μM
Incubation Time:

24 hours
Result:

Increased the percentage of S stage in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

SK-OV-3 cells
Concentration:

5.0 and 10 μM
Incubation Time:

24 hours
Result:

Decreased the expression of antiapoptotic protein Bcl-2, while increased pro-apoptotic Bax and caspase expression.

In Vivo

Antitumor agent-61 (compound 6b) (10-20 mg/kg; i.h.; Twice daily, for 28 days; BALB/c nude mice with SK-OV-3 xenograft) reduces mean NPC tumor burden in a dose-dependent manner^[1].

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

Animal Model:

BALB/c nude mice with SK-OV-3 xenograft^[1]
Dosage:

10 and 20 mg/kg
Administration:

Subcutaneous injection; Twice daily, for 28 days.
Result:

Suppressed tumor growth by 47.7% and 56.8% for 10 and 20 mg/kg, respectively, without affecting body weight or causing any overt adverse effects.

Chemical Information

CAS No. 2408917-12-2
Molecular Weight 992.08
Formula C₅₄H₆₃FN₅O₁₀P
SMILES

O=C(N1CCC(CC1)N2CCCCC2)OC3=CC4=C(CC)C5=C(C6=CC7=C(COC(C7(CC)OC(CCCC8=CC=C(NC(P(OCC)(OCC)=O)C9=CC=C(C=C9)F)C=C8)=O)=O)C(N6C5)=O)N=C4C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 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)
Handling Instructions (2659 KB)

References

[1]. Xiaochao Huang, et al. Synthesis, mechanisms of action, and toxicity of novel aminophosphonates derivatives conjugated irinotecan in vitro and in vivo as potent antitumor agents. Eur J Med Chem. 2020 Mar 1;189:112067. [Content Brief]

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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.

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