CM-272
- Product Name
- CM-272
- CAS No.
- 1846570-31-7
- Chemical Name
- CM-272
- Synonyms
- CM-272;CM-272; CM 272; CM272;6-Methoxy-2-(5-methylfuran-2-yl)-N-(1-methylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinolin-4-amine;4-Quinolinamine, 6-methoxy-2-(5-methyl-2-furanyl)-N-(1-methyl-4-piperidinyl)-7-[3-(1-pyrrolidinyl)propoxy]-;DNMT1,anti-tumour,DNMTs,immunogenic,DNA MTases,CM272,DNMT3A,CM 272,G9a,H3K9me2,Inhibitor,epigenetics,Histone Methyltransferase,GLP,Apoptosis,inhibit,substrate-competitive,CM-272,DNMT3B,DNA Methyltransferase
- CBNumber
- CB14632529
- Molecular Formula
- C28H38N4O3
- Formula Weight
- 478.63
- MOL File
- 1846570-31-7.mol
CM-272 Property
- Boiling point:
- 631.9±55.0 °C(Predicted)
- Density
- 1.164±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:84.0(Max Conc. mg/mL);179.5(Max Conc. mM)
Ethanol:63.0(Max Conc. mg/mL);131.63(Max Conc. mM) - form
- A crystalline solid
- pka
- 10.09±0.20(Predicted)
- color
- Light brown to brown
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- Axon2812
- Product name
- CM-272
- Purity
- 98%
- Packaging
- 5mg
- Price
- $137.5
- Updated
- 2021/12/16
- Product number
- CS-0022181
- Product name
- CM-272
- Purity
- 98.13%
- Packaging
- 5mg
- Price
- $220
- Updated
- 2021/12/16
- Product number
- CS-0022181
- Product name
- CM-272
- Purity
- 98.13%
- Packaging
- 10mg
- Price
- $375
- Updated
- 2021/12/16
- Product number
- CS-0022181
- Product name
- CM-272
- Purity
- 98.13%
- Packaging
- 50mg
- Price
- $950
- Updated
- 2021/12/16
- Product number
- CS-0022181
- Product name
- CM-272
- Purity
- 98.13%
- Packaging
- 100mg
- Price
- $1350
- Updated
- 2021/12/16
CM-272 Chemical Properties,Usage,Production
Biological Activity
CM272 is a novel, first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 values of 8 nM, 382 nM, 85 nM, 1200 nM, and 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, and GLP, respectively. CM272 prolongs survival in in vivo models of hematological malignancies by at least partially inducing immunogenic cell death.
in vitro
CM-272 (100-1000 nM; 12-72 hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment inhibits cell proliferation in a dose- and time-dependent manner.
CM-272 (100-1000 nM; 24 hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment blocks cell cycle progression.
CM-272 (100-1000 nM; 12-72 hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment induces apoptosis in ALL, AML and DLBCL cell lines in a dose- and time-dependent manner.
CM-272 after 48 h of treatment CEMO -1 acute lymphoblastic leukaemia (ALL) cell line, MV4-11 acute myeloid leukaemia (AML) cell line and OCI-Ly10 diffuse large B-cell lymphoma (DLBCL) cell line, the GI 50 values of 218 nM, 269 nM and 455 nM, respectively, and is associated with a decrease in global levels of H3K9me2 and 5mC.
The therapeutic activity of CM-272 relies on the early activation of the type I IFN response in tumour cells , potentially leading to the induction of cell autonomous immunogenic death in tumou r cells.
Cell Proliferation Assay
Cell Line: | CEMO-1, MV4-11 and OCI-Ly10 cell lines |
Concentration: | 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 Time: | 12 hours, 24 hours, 48 hours and 72 hours |
Result: | Inhibited cell proliferation in a dose- and time-dependent manner. |
Cell Cycle Analysis
Cell Line: | CEMO-1, MV4-11 and OCI-Ly10 cell lines |
Concentration: | |
Concentration: td> | 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 Time: | 24 hours |
Result: | Blocked cell cycle progression. |
Apoptosis Analysis
Cell Line: | CEMO-1, MV4-11 and OCI-Ly10 cell lines |
Concentration: | 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 Time: | 12 hours, 24 hours, 48 hours and 72 hours | Result: | Induced apoptosis in ALL, AML and DLBCL cell lines in a dose- and time-dep endent manner. |
in vivo
CM-272 (2.5 mg/kg; injection; daily; for 28 days; female Rag2 intravenous ?/? γc ?/? mice) treatment significantly prolongs survival of CEMO-1 cells xenogeneic models.
Animal Model: | Female BALB/Ca-Rag2 ?/? γc ?/? mice (6–8-week-old) with CEMO-1 cells |
Dosage: | 2.5 mg/kg |
Administration: | Intravenous injection; daily; for 28 days |
Result: | Induced a statistically significant increase in overall survival (OS) in mice. |
target
Target | Value |
G9a (Cell-free assay) | 8 nM |
DNMT3A (Cell-free assay) | 85 nM |
382 nM | |
DNMT3B (Cell-free assay) td> | 1200 nM |
CM-272 Preparation Products And Raw materials
Raw materials
Preparation Products
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