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Antitumor agent-101
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Catalog No. T79249Cas No. 2848632-52-8
Antitumor agent-101 is a selective, covalent inhibitor targeting lysine methyltransferases G9a/GLP, demonstrating IC50 values of 8.5 nM for G9a and 5.5 nM for GLP. It exhibits antitumor efficacy in the PANC-1 xenograft model [1].
Antitumor agent-101
😃Good
Catalog No. T79249Cas No. 2848632-52-8
Antitumor agent-101 is a selective, covalent inhibitor targeting lysine methyltransferases G9a/GLP, demonstrating IC50 values of 8.5 nM for G9a and 5.5 nM for GLP. It exhibits antitumor efficacy in the PANC-1 xenograft model [1].
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $1,520 | 8-10 weeks | |
| 50 mg | $1,980 | 8-10 weeks | |
| 100 mg | $2,500 | 8-10 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| Description | Antitumor agent-101 is a selective, covalent inhibitor targeting lysine methyltransferases G9a/GLP, demonstrating IC50 values of 8.5 nM for G9a and 5.5 nM for GLP. It exhibits antitumor efficacy in the PANC-1 xenograft model [1]. |
| Targets&IC50 | G9a:8.5 nM, GLP:5.5 nM |
| In vitro | Antitumor agent-101 (Compound 27) (0-5 μM; 48 hours) inhibits proliferation and colony formation in PANC-1 and MDA-MB-231 cells [1]. Furthermore, Antitumor agent-101 (0-10 μM; 0-96 hours) effectively reduces H3K9me2 levels in these cells in a concentration- and time-dependent manner. |
| In vivo | Antitumor agent-101 (Compound 27), administered at 2 mg/kg via intraperitoneal injection five times per week, inhibits the growth of PANC-1 xenograft tumors by suppressing the methyltransferase activity of G9a/GLP [1]. Additionally, this compound demonstrates a peak plasma concentration (Cmax) of 316 ng/mL and a mean residence time (MRT) of 0.61 hours [1]. |
| Molecular Weight | 482.62 |
| Formula | C26H38N6O3 |
| Cas No. | 2848632-52-8 |
Storage & Solubility Information
| Storage | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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