CM272

製品コードS8812 バッチS881202

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C28H38N4O3

 
分子量 478.63 CAS No. 1846570-31-7
Solubility (25°C)* 体外 DMSO 96 mg/mL (200.57 mM)
Ethanol 96 mg/mL (200.57 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5% DMSO 95% Corn oil
0.6mg/ml Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.85mg/ml Taking the 1 mL working solution as an example, add 50 μL of 97 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 CM-272 is a novel first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 of 8 nM, 382 nM, 85 nM, 1200 nM, 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, GLP, respectively. CM-272 prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death.
in vitro

The GI50 for CM-272 after 48 h of treatment in ALL, AML and DLBCL-derived cell lines is in the nM range and is associated with a decrease in global levels of H3K9me2 and 5mC. CM-272 inhibits cell proliferation, blocks cell cycle progression and induces apoptosis in ALL, AML and DLBCL cell lines in a dose-dependent manner. CM-272 induces IFN response and immunogenic cell death.[1].
in vivo

CM272 therapy induces a statistically significant increase in overall survival (OS) in mice in comparison with control animals. Global H3K9me2 and 5mC levels are reduced in leukaemic cells obtained from mice engrafted with ALL-derived CEMO-1 cells after 1 week of treatment and no significant weight loss is observed in treated animals. CM272 shows dose-dependent efficacy and a dose of 2.5 mg/kg of CM272 is adequate to demonstrate the positive anti-tumour efficacy in mice engrafted with ALL-derived CEMO-1 cells.[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 ALL, AML, DLBCL, CEMO-1, LAL-CUN-2, MV4-11, OCI-AML-2, OCI-Ly3, OCI-Ly10 cell lines
濃度 --
反応時間 24, 48, 72 and 96h
実験の流れ

"100.000 cells of CEMO-1, LAL-CUN-2, MV4-11 and OCI-AML-2 cell lines are cultured at a density of 1x106 cells/mL and treated for 12, 24, 48 and 72 hours with CM-272 at different concentrations (GI25, GI50 and GI75). In the case of OCI-Ly3 and OCI-Ly10, cells are treated with 100, 400 and 1000 nM for 24, 48, 72 and 96h. Cells are washed twice with phosphatebuffered saline (PBS) and resuspended in 1X Binding Buffer at a concentration of 1x106 cells/mL. 1 µL of FITC Annexin V antibody and 2 µL of propidium iodide are added and incubated for 15 min at RT in the dark. Finally, 400 µL of 1X Binding Buffer are added to each tube and analyzed by flow cytometry within 1 h. "
動物実験 動物モデル 6–8-week-old female BALB/cA−Rag2 γc mice
投薬量 1, 2.5 mg/kg
投与方法 IV

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Targeting G9a/DNMT1 methyltransferase activity impedes IGF2-mediated survival in hepatoblastoma [ Hepatol Commun, 2024, 8(2)e0378] PubMed: 38285887
Inhibition of a G9a/DNMT network triggers immune-mediated bladder cancer regression [ Nat Med, 2019, 25(7):1073-1081] PubMed: 31270502

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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