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| 2mg |
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Purity: ≥98%
CM-272 (CM272) is a first-in-class, reversible, and dual inhibitor of G9a and DNMTs in hematological malignancies with antineoplastic effects. In vitro treatment of haematological neoplasia (acute myeloid leukaemia-AML, acute lymphoblastic leukaemia-ALL and diffuse large B-cell lymphoma-DLBCL) with CM-272 indicate that CM-272 inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death. It significantly prolongs survival of AML, ALL and DLBCL xenogeneic models. CM-272 is a promising therapeutic tool for unmet needs in haematological tumors.
| ln Vitro |
Treatment with CM-272 (100-1000 nM; 12-72 hours; CEMO-1, MV4-11, and OCI-Ly10 cell lines) suppresses cell growth in a time- and dose-dependent fashion [1]. Cell cycle progression is blocked by CM-272 treatment (100-1000 nM; 24-hour; CEMO-1, MV4-11, and OCI-Ly10 cell lines) [1]. In ALL, AML, and DLBCL cell lines, CM-272 (100–1000 nM; 12-72 hours; CEMO-1, MV4-11, and OCI-Ly10 cell lines) treatment causes apoptosis in a time- and dose-dependent manner[1]. 48 hours following treatment of the CEMO-1 acute lymphoblastic leukemia (ALL), MV4-11 acute myeloid leukemia (AML), and OCI-Ly10 cell line, the CM-272 diffuse large B-cell lymphoma (DLBCL) cell line showed reduced overall levels of H3K9me2 and 5mC (GI50 values of 218 nM, 269 nM, and 455 nM, respectively [1]. The processing activity of CM-272 is dependent on the early generation of type I interferon responses in tumor cells, which may cause the cells to undergo cell-autonomous immunogenic death [1].
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| ln Vivo |
Treatment with CM-272 (2.5 mg/kg; intravenously; daily; for 28 days; female Rag2/γc/mouse) considerably extended the CEMO-1 cell xenogeneic model [1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: CEMO-1, MV4-11 and OCI-Ly10 cell lines Tested Concentrations: 125 nM, 250 nM, 500 nM (CEMO-1 cells); 135 nM, 270 nM, 540 nM (MV4- 11 cells); 100 nM, 400 nM, 1000 nM (OCI-Ly10 cells) Incubation Duration: 12 hrs (hours), 24 hrs (hours), 48 hrs (hours) and 72 hrs (hours) Experimental Results: Inhibited cell proliferation in a dose- and time-dependent manner. Cell Cycle Analysis [1] Cell Types: CEMO-1, MV4-11 and OCI-Ly10 cell lines Tested Concentrations: 125 nM, 250 nM, 500 nM (CEMO-1 cells); 135 nM, 270 nM, 540 nM (MV4-11 cells) ; 100 nM, 400 nM, 1000 nM (OCI-Ly10 cells) Incubation Duration: 24 hrs (hours) Experimental Results: Blocked cell cycle progression. Apoptosis Analysis[1] Cell Types: CEMO-1, MV4-11 and OCI-Ly10 cell lines Tested Concentrations: 125 nM, 250 nM, 500 nM (CEMO-1 cells); 135 nM, 270 nM, 540 nM (MV4-11 cells); 100 nM, 400 nM, 1000 nM (OCI-Ly10 cells) Incubation Duration: 12 hrs (hours), 24 hrs (hours), 48 hrs (hours) and 72 hrs (hours) Experimental Results: Induced apoptosis in ALL, AML and DLBCL cell lines in a dose- and time-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Female BALB/Ca-Rag2−/−γc−/− mice (6–8weeks old) with CEMO-1 cells[1]
Doses: 2.5 mg/kg Route of Administration: intravenous (iv) injection; daily; for 28 days Experimental Results: Induced a statistically significant increase in overall survival (OS) in mice. |
| References | |
| Additional Infomation |
CM-272 is a member of the class of aminoquinolines that is is quinoline substituted by 5-methylfuran-2-yl, (1-methylpiperidin-4-yl)amino, methoxy, and 3-(pyrrolidin-1-yl)propoxy groups at positions 2, 4, 6 and 7, respectively. It is a dual G9a/DNA methyltransferases inhibitor with antitumor activity. It inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP (IC50 = 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively). It has a role as an apoptosis inducer, a ferroptosis inducer, an antineoplastic agent, an EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor and an EC 2.1.1.37 [DNA (cytosine-5-)-methyltransferase] inhibitor. It is a N-alkylpyrrolidine, a member of furans, an aminoquinoline, an aromatic ether, a member of piperidines, a tertiary amino compound, a secondary amino compound and a diether.
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| Molecular Formula |
C28H38N4O3
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| Molecular Weight |
478.64
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| Exact Mass |
478.294
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| CAS # |
1846570-31-7
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| Related CAS # |
1846570-31-7;1846570-32-8 (TFA);
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| PubChem CID |
118607432
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| Appearance |
Light brown to brown solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
631.9±55.0 °C at 760 mmHg
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| Flash Point |
336.0±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.601
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| LogP |
5.41
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
35
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| Complexity |
640
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RLQLKZTYUYIWDB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H38N4O3/c1-20-7-8-26(35-20)25-18-23(29-21-9-14-31(2)15-10-21)22-17-27(33-3)28(19-24(22)30-25)34-16-6-13-32-11-4-5-12-32/h7-8,17-19,21H,4-6,9-16H2,1-3H3,(H,29,30)
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| Chemical Name |
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0893 mL | 10.4463 mL | 20.8925 mL | |
| 5 mM | 0.4179 mL | 2.0893 mL | 4.1785 mL | |
| 10 mM | 0.2089 mL | 1.0446 mL | 2.0893 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Small molecules with a dual inhibitory activity against G9a and DNMT.Nat Commun.2017 May 26;8:15424. |
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CM-272inhibits cell proliferation and induces apoptosis.Nat Commun.2017 May 26;8:15424. |
CM-272induces type I IFN response and immunogenic cell death.Nat Commun.2017 May 26;8:15424. |
CM-272shows anti-leukaemic effectsin vivo.Nat Commun.2017 May 26;8:15424. |
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