CM-272 |
カタログ番号GC12367
One-Click Copy Product Info
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CM-272 は、抗腫瘍活性を備えたクラス初の強力な選択的基質競合性可逆デュアル G9a/DNA メチルトランスフェラーゼ (DNMT) 阻害剤です。 CM-272 は、G9a、DNMT1、DNMT3A、DNMT3B、および GLP を、それぞれ 8 nM、382 nM、85 nM、1200 nM、および 2 nM の IC50 で阻害します。 CM-272 は細胞増殖を阻害し、アポトーシスを促進し、IFN 刺激遺伝子と免疫原性細胞死を誘導します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1846570-31-7
Sample solution is provided at 25 µL, 10mM.
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CM-272 is a first-in-class reversible dual inhibitor against G9a and DNMTs with IC50 values of 8 nM and 382 nM, respectively [1].
G9a is a histone methyltransferase that is overexpressed in many tumors. Inhibition of G9a expression reduces cancer cell proliferation, delays disease progression and inhibits tumor metastasis. G9a interacts with DNA methyltransferase-1 (DNMT1) to coordinate DNA and histone methylation during cell division promoting transcriptional silencing of target genes. Reduction of both DNA and H3K9 methylation levels leads to reactivation of tumor suppressor genes and inhibits cancer cell proliferation [1].
CM-272 is a first-in-class reversible and substrate-competitive dual inhibitor of G9a and DNMTs. In ALL, AML and DLBCL-derived cell lines, CM-272 reduced DNA methylation in the promoter region of specific tumor suppressor genes. CM-272 also inhibited cell proliferation, blocked cell cycle progression and induced apoptosis in a dose-dependent way [1].
In immunodeficient Rag2-/-γc-/- mice injected i.v. with ALL-derived CEMO cells, CM-272 significantly increased overall survival (OS) in mice (median OS; 92±5.7 days versus 55±10.5 days; P=0.0009) without significant weight loss. In immunodeficient Rag2-/-γc-/- mice injected i.v. with AML-derived MV4-11 cells, CM-272 also prolonged OS in mice. CM-272 exerted a potent anti-tumour activity in vivo against different types of haematological malignancies by inhibiting the methyltransferase activity of both G9a/GLP and DNMTs [1].
Reference:
[1]. San José-Enériz E, Agirre X, Rabal O, et al. Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies. Nat Commun. 2017 May 26;8:15424. doi: 10.1038/ncomms15424.
| Cas No. | 1846570-31-7 | SDF | |
| Chemical Name | 6-methoxy-2-(5-methylfuran-2-yl)-N-(1-methylpiperidin-4-yl)-7-(3-(pyrrolidin-1-yl)propoxy)quinolin-4-amine | ||
| Canonical SMILES | COC1=C(C=C(N=C(C2=CC=C(C)O2)C=C3NC4CCN(C)CC4)C3=C1)OCCCN5CCCC5 | ||
| Formula | C28H38N4O3 | M.Wt | 478.63 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:6): 0.15 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0893 mL | 10.4465 mL | 20.893 mL |
| 5 mM | 417.9 μL | 2.0893 mL | 4.1786 mL |
| 10 mM | 208.9 μL | 1.0446 mL | 2.0893 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)