Antitumor agent-101
Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model.
For research use only. We do not sell to patients.
- CAS No.: 2848632-52-8
- Formula: C26H38N6O3
- Molecular Weight:482.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
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G9a 8.5 nM (IC50) |
GLP 5.5 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
2.88 μM
Compound: 27
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Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability measured after 24 hrs by CCK-8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability measured after 24 hrs by CCK-8 assay
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[PMID: 37268593] |
| PANC-1 | IC50 |
2.68 μM
Compound: 27
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Antiproliferative activity against human PANC-1 cells assessed as cell viability measured after 24 hrs by CCK-8 assay
Antiproliferative activity against human PANC-1 cells assessed as cell viability measured after 24 hrs by CCK-8 assay
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[PMID: 37268593] |
Antitumor agent-101 (Compound 27) ( 0-5 μM; 48 hours) significantly exhibits proliferation and colony formation of PANC-1 and MDA-MB-231 cells with IC50s of 2.68 and 2.88 μM, respectively[1].
Antitumor agent-101 (0-10 μM; 0-96 hours) effectively reduces H3K9me2 in PANC-1 and MDA-MB-231 cells in a concentration- and time-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PANC-1 and MDA-MB-231 cells
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Concentration:0, 1.25, 2.5, 5 μM
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Incubation Time:48 hours
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Result:Ihibited proliferation of PANC-1 and MDA-MB-231 cells with IC50s of 2.68 and 2.88 μM, respectively.
Significantly suppressed the colony formation in MDA-MB-231 and PANC-1 cell lines at 2.5 μM.
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Cell Line:PANC-1 and MDA-MB-231 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:4, 48, 72, or 96 hours
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Result:Effectively reduced H3K9me2 in PANC-1 and MDA-MB-231 cells in a concentration- and time-dependent manner.
Still significantly inhibited the levels of H3K9me2 in the cells treated with compound 27 were still significantly inhibited within 24h after Antitumor agent-101 was washed out, and the levels of H3K9me2 were recovered after 48h.
Antitumor agent-101 (2 mg/kg for p.o.) shows a Cmax of 316 ng/mL, and mean residence time (MRT) of 0.61 hour[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:PANC-1 xenograft tumor models in male Balb/c nu/nu mice[1]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection (i.p.), 5 days a week (5 days on and 2 days off).
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Result:Exhibited potent antitumor activity with a tumor growth inhibition (TGI) rate of 52.2% with no obvious toxicity.
Showed lower levels of H3K9me2 than the vehicle group.
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Animal Model:Male ICR Mice (Pharmacokinetic assay)[1]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Pharmacokinetic parameters for antitumor agent-101 (Compound 27) in rats [1]
Route Dose (mg/kg) Cmax (ng/mL) AUC0-t (h•ng/mL) AUC0-Ꝏ (h•ng/mL) MRT (h) i.p. 2 316 208 214 0.61 
Chemical Information
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CAS No. 2848632-52-8
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Molecular Weight 482.62
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Formula C26H38N6O3
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SMILES
COC1=CC2=C(N=C(N(C)C(C=C)=O)N=C2NC3CCN(C)CC3)C=C1OCCCN4CCCC4
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Shipping
Room temperature in continental US; may vary elsewhere.
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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%
References
Calculators
Molarity CalculatorMass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)= × ×Dilution CalculatorConcentration (start) × Volume (start) = Concentration (final) × Volume (final)
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Antitumor agent-101 Related Classifications
HY-155020 Related Classifications
Keywords
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