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MPI-0479605

Product Name
MPI-0479605
CAS No.
1246529-32-7
Chemical Name
MPI-0479605
Synonyms
CS-1459;MPI-0479605;MPI0479605 HCl;MPI-0479605 USP/EP/BP;MPI-0479605 (MPI0479605);MPI-0479605, 10 mM in DMSO;MPI-0479605;MPI 0479605;MPI0479605;N6-cyclohexyl-N2-(2-methyl-4-morpholinophenyl)-9H-purine-2,6-diamine;N6-Cyclohexyl-N2-[2-methyl-4-(4-morpholinyl)phenyl]-9H-purine-2,6-diamine;9H-?Purine-?2,?6-?diamine, N6-?cyclohexyl-?N2-?[2-?methyl-?4-?(4-?morpholinyl)?phenyl]?-
CBNumber
CB32731101
Molecular Formula
C22H29N7O
Formula Weight
407.51
MOL File
1246529-32-7.mol
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MPI-0479605 Property

Boiling point:
745.8±70.0 °C(Predicted)
Density 
1.318±0.06 g/cm3(Predicted)
storage temp. 
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
solubility 
Soluble in DMSO
form 
A crystalline solid
pka
10.52±0.10(Predicted)
color 
White to gray
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H226Flammable liquid and vapour

Precautionary statements

P210Keep away from heat/sparks/open flames/hot surfaces. — No smoking.

P233Keep container tightly closed.

P240Ground/bond container and receiving equipment.

P241Use explosion-proof electrical/ventilating/lighting/…/equipment.

P242Use only non-sparking tools.

P243Take precautionary measures against static discharge.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P303+P361+P353IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.

P370+P378In case of fire: Use … for extinction.

P403+P235Store in a well-ventilated place. Keep cool.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
22136
Product name
MPI-0479605
Purity
≥98%
Packaging
1mg
Price
$57
Updated
2024/03/01
Cayman Chemical
Product number
22136
Product name
MPI-0479605
Purity
≥98%
Packaging
5mg
Price
$233
Updated
2024/03/01
Cayman Chemical
Product number
22136
Product name
MPI-0479605
Purity
≥98%
Packaging
10mg
Price
$437
Updated
2024/03/01
Cayman Chemical
Product number
22136
Product name
MPI-0479605
Purity
≥98%
Packaging
25mg
Price
$957
Updated
2024/03/01
Adipogen Life Sciences
Product number
SYN-1187-M001
Product name
MPI-0479605hydrochloride
Purity
≥95%
Packaging
1mg
Price
$205
Updated
2021/12/16
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MPI-0479605 Chemical Properties,Usage,Production

Description

MPI-0479605 is a potent and ATP-competitive inhibitor of the mitotic kinase MPS1 (IC50 = 1.8 nM). It is selective for MPS1 over a panel of 79 kinases at a concentration of 500 nM. MPI-0479605 induces time-dependent degradation of cyclin B and securin and decreases phosphorylation of BUBR1 resulting in failed cytokinesis in HeLa cells arrested by nocodazole . It also causes misalignment of chromosomes at the anaphase plate and aneuploidy in A549 cells and slows cell cycle progression of HCT116 and COLO 205 cells irrespective of p53 activity. MPI-0479605 (30-150 mg/kg) reduces tumor volume in an HCT116 mouse colon cancer xenograft model in a dose-dependent manner.

Uses

MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM.

Synthesis

39639-45-7

1246532-35-3

1246529-32-7

The general procedure for the synthesis of N6-cyclohexyl-N2-(2-methyl-4-morpholinophenyl)-9H-purine-2,6-diamine from compound (CAS:39639-45-7) and compound (CAS:1246532-35-3) was as follows: compound 1 (2.00 g, 7.91 mmol) was mixed with compound 4 (2.53 g, 9.56 mmol), sodium acetate (980 mg, 11.95 mmol) and chloroform (40 mL) in an 80 mL microwave reaction flask to form a suspension. Subsequently, the mixture was heated to 150 °C in a microwave reactor and maintained for 30 min. Upon completion of the reaction, the solvent was removed by distillation under reduced pressure. The resulting crude product was purified by reversed-phase medium pressure liquid chromatography (MPLC) to give a final white solid product in 12-30% yield.

in vivo

MPI-0479605 (30 mg/kg daily or 150 mg/kg every fourth day (Q4D), i.p.) inhibits tumor growth by 49% and 74 % in HCT-116 xenografts. However, MPI-0479605 does not show inhibitory activity via daily dosing on the Colo-205 xenografts, and dosing every four days causes 63% tumor growth inhibition (TGI)[1].

IC 50

Mps1: 1.8 nM (IC50); ALK: 0.26 μM (IC50); B-RAF: 3.2 μM (IC50); ERK2: 3.9 μM (IC50); FAK1: 2.7 μM (IC50); FER: 0.59 μM (IC50); FLT3: 0.08 μM (IC50); INSR: 0.38 μM (IC50); JNK1: 0.11 μM (IC50); PLK4: 3.3 μM (IC50); STK33: 1.1 μM (IC50)

References

[1] tardif k d, rogers a, cassiano j, et al. characterization of the cellular and antitumor effects of mpi-0479605, a small-molecule inhibitor of the mitotic kinase mps1. molecular cancer therapeutics, 2011, 10(12): 2267-2275.

MPI-0479605 Preparation Products And Raw materials

Raw materials

Preparation Products

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MPI-0479605 Suppliers

China 94 India 1 United Kingdom 1 United States 11 Global 107
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
Advantage
58
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
Country
China
ProdList
9510
Advantage
58
Jiangsu Aikon Biopharmaceutical R&D co.,Ltd.
Tel
025-66113011 17798518460
Fax
(1)02557626880
Email
cfzhang@aikonchem.com
Country
China
ProdList
19913
Advantage
55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
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55
Shanghaizehan biopharma technology co., Ltd.
Tel
021-61350663 13052117465
Fax
021-61350662
Email
sales@zehanbiopharma.com
Country
China
ProdList
984
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55
D&C Chemicals
Tel
+86-21-58447131
Fax
+86-21-61642470
Email
1724405207@qq.com
Country
China
ProdList
472
Advantage
55
Guangzhou Zhiya Chemdrugs Co.,Ltd
Tel
18122150900
Fax
QQ:2869377561
Email
sculk28@163.com
Country
China
ProdList
646
Advantage
55
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View Lastest Price from MPI-0479605 manufacturers

Career Henan Chemical Co
Product
MPI-0479605 1246529-32-7
Price
US $1.00/KG
Min. Order
1KG
Purity
97%-99.9%
Supply Ability
100kg
Release date
2019-12-25

1246529-32-7, MPI-0479605Related Search:

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  • MPI-0479605
  • N6-cyclohexyl-N2-(2-methyl-4-morpholinophenyl)-9H-purine-2,6-diamine
  • MPI0479605 HCl
  • N6-Cyclohexyl-N2-[2-methyl-4-(4-morpholinyl)phenyl]-9H-purine-2,6-diamine
  • MPI-0479605;MPI 0479605;MPI0479605
  • 9H-?Purine-?2,?6-?diamine, N6-?cyclohexyl-?N2-?[2-?methyl-?4-?(4-?morpholinyl)?phenyl]?-
  • CS-1459
  • MPI-0479605 USP/EP/BP
  • MPI-0479605, 10 mM in DMSO
  • MPI-0479605 (MPI0479605)
  • 1246529-32-7
  • C22H29N7O
  • Inhibitors