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
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
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..…
N-Bromosuccinimide Price
- Product number
- 22136
- Product name
- MPI-0479605
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $57
- Updated
- 2024/03/01
- Product number
- 22136
- Product name
- MPI-0479605
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $233
- Updated
- 2024/03/01
- Product number
- 22136
- Product name
- MPI-0479605
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $437
- Updated
- 2024/03/01
- Product number
- 22136
- Product name
- MPI-0479605
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $957
- Updated
- 2024/03/01
- Product number
- 2574AH
- Product name
- N6-Cyclohexyl-N2-(2-methyl-4-morpholinophenyl)-9H-purine-2,6-diamine
- Packaging
- 1g
- Price
- $1246
- Updated
- 2021/12/16
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
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View Lastest Price from MPI-0479605 manufacturers
- 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