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CM-272

Product Name
CM-272
CAS No.
1846570-31-7
Chemical Name
CM-272
Synonyms
CM-272;CM-272, 10 mM in DMSO;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
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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
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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.

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N-Bromosuccinimide Price

Axon Medchem
Product number
Axon2812
Product name
CM-272
Purity
98%
Packaging
5mg
Price
$137.5
Updated
2021/12/16
ChemScene
Product number
CS-0022181
Product name
CM-272
Purity
98.13%
Packaging
5mg
Price
$220
Updated
2021/12/16
ChemScene
Product number
CS-0022181
Product name
CM-272
Purity
98.13%
Packaging
10mg
Price
$375
Updated
2021/12/16
ChemScene
Product number
CS-0022181
Product name
CM-272
Purity
98.13%
Packaging
50mg
Price
$950
Updated
2021/12/16
ChemScene
Product number
CS-0022181
Product name
CM-272
Purity
98.13%
Packaging
100mg
Price
$1350
Updated
2021/12/16
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CM-272 Chemical Properties,Usage,Production

Uses

CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death[1].

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: 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

< tr>
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

< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> DNMT1
(Cell-free assay)
TargetValue
G9a
(Cell-free assay)		 8 nM
DNMT3A
(Cell-free assay)		 85 nM
382 nM
DNMT3B
(Cell-free assay)		 1200 nM

IC 50

G9a: 8 nM (IC50); EHMT1/GLP/KMT1D: 2 nM (IC50); DNMT1: 382 nM (IC50); DNMT3A: 85 nM (IC50); DNMT3B: 1200 nM (IC50)

References

[1] San José-Enériz E, 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

CM-272 Preparation Products And Raw materials

Raw materials

Preparation Products

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CM-272 Suppliers

CHINA 62 United States 7 Global 69
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
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United States
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12952
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Bide Pharmatech Ltd.
Tel
400-400-164-7117 18317119277
Fax
+86-21-61629029
Email
product02@bidepharm.com
Country
China
ProdList
40000
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60
Shanghai Macklin Biochemical Co.,Ltd.
Tel
15221275939
Fax
021-50706099
Email
shenlinxing@macklin.cn
Country
China
ProdList
15872
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55
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4795
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Shanghai Beckham Medical Technology Co., Ltd
Tel
13816613772
Fax
QQ: 12922499
Email
huahero21@sina.com
Country
China
ProdList
2495
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55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
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58
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
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ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8000
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62
Shanghai SuperLan Chemcial Technique Centre
Tel
0-2022843681 15618226720
Fax
+86-21-51601218
Email
chaolaichem@foxmail.com
Country
China
ProdList
10408
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Beijing Jin Ming Biotechnology Co., Ltd.
Tel
010-60605840 18892239720
Fax
010-60605840
Email
psaitong@jm-bio.com
Country
China
ProdList
12306
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58

1846570-31-7, CM-272Related Search:


  • CM-272; CM 272; CM272
  • CM-272
  • 4-Quinolinamine, 6-methoxy-2-(5-methyl-2-furanyl)-N-(1-methyl-4-piperidinyl)-7-[3-(1-pyrrolidinyl)propoxy]-
  • 6-Methoxy-2-(5-methylfuran-2-yl)-N-(1-methylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinolin-4-amine
  • 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
  • CM-272, 10 mM in DMSO
  • 1846570-31-7