PRT-060318
- Product Name
- PRT-060318
- CAS No.
- 1194961-19-7
- Chemical Name
- PRT-060318
- Synonyms
- CS-1688;PRT 318;P 142-76;PRT-060318;PRT-060318 ≥95%;PRT-060318(PRT318);PRT 060318 ;PRT060318;PRT 318;PRT-318;PRT318;2-(((1R,2S)-2-aminocyclohexyl)amino)-4-(m-tolylamino)pyrimidine-5-carboxamide;4-(3-methyl-phenyl-amino-)-2-(2-amino-cyclo-hexyl-amino-)-pyrimidine-5-carboxamide;2-[[(1R,2S)-2-Aminocyclohexyl]amino]-4-[(3-methylphenyl)amino]-5-pyrimidinecarboxamide
- CBNumber
- CB12731127
- Molecular Formula
- C18H24N6O
- Formula Weight
- 340.42
- MOL File
- 1194961-19-7.mol
PRT-060318 Property
- Melting point:
- 152 - 155°C
- Boiling point:
- 602.1±65.0 °C(Predicted)
- Density
- 1.277±0.06 g/cm3(Predicted)
- storage temp.
- Refrigerator, under inert atmosphere
- solubility
- DMSO (Slightly), Methanol (Slightly)
- pka
- 14.10±0.50(Predicted)
- form
- Solid
- color
- Pale Brown
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H242Heating may cause a fire
- Precautionary statements
-
P210Keep away from heat/sparks/open flames/hot surfaces. — No smoking.
P234Keep only in original container.
P235Keep cool.
P240Ground/bond container and receiving equipment.
P370+P378In case of fire: Use … for extinction.
P403Store in a well-ventilated place.
N-Bromosuccinimide Price
- Product number
- SML2505
- Product name
- PRT-060318
- Purity
- ≥95% (HPLC)
- Packaging
- 5mg
- Price
- $123
- Updated
- 2024/03/01
- Product number
- SML2505
- Product name
- PRT-060318
- Purity
- ≥95% (HPLC)
- Packaging
- 25mg
- Price
- $347
- Updated
- 2024/03/01
- Product number
- 22476
- Product name
- PRT060318
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $144
- Updated
- 2024/03/01
- Product number
- 22476
- Product name
- PRT060318
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $274
- Updated
- 2024/03/01
- Product number
- 22476
- Product name
- PRT060318
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $502
- Updated
- 2024/03/01
PRT-060318 Chemical Properties,Usage,Production
Description
PRT060318 is a potent and selective inhibitor of spleen tyrosine kinase (Syk; IC50 = 4 nM). It is selective, inhibiting 92% of Syk activity, while other kinases retain >70% activity, at a concentration of 50 nM in a panel of 270 kinases. PRT060318 inhibits convulxin-induced aggregation of human platelet-rich plasma (IC50 = 2.5 μM) in vitro and prevents thrombosis in a transgenic mouse model of heparin-induced thrombocytopenia. It induces chronic lymphocytic leukemia (CLL) B cell apoptosis and inhibits the secretion of chemokines CCL3, CCL4, and CXCL13. PRT060318 also inhibits CLL B cell chemotaxis and pseudoemperipolesis.
Uses
PRT 060318 is a novel selective inhibitor of the tyrosine kinase Syk. PRT 060318 may be used in Heparin-Induced Thrombocytopenia (HIT) treatment. HIT is a major cause of morbidity and mortality.
in vitro
prt-060318 was identified as a potent inhibitor of purified syk kinase. syk kinase was inhibited by 92%, while the activities all other kinases retained more than 70% when prt-060318 were evaluated at a concentration of 50 nm in a broad panel of kinase enzyme assays. in addition, prt-060318 could dose-responsively inhibited convulxin-induced human prp aggregation. moreover, it was found that prt-060318 was able to dose-responsively inhibit the increases in intracellular calcium in convulxin-treated platelets [1].
in vivo
animal study showed that in contrast to vehicle-treated mice developed the expected thrombocytopenia, prt-060318-treated mice had no significant change in platelet counts after injection of heparin. moreover, the nadir platelet counts of prt-060318-treated mice were found to be significantly higher than control mice. the prt-060318-treated mice showed no bleeding diathesis or other adverse effects. in addition, prt-060318 treatment in crush thrombosis model resulted in significant inhibition of platelet deposition without changing bleeding time [1].
IC 50
4 nm
References
[1] reilly mp,sinha u,andré p,taylor sm,pak y,deguzman fr,nanda n,pandey a,stolla m,bergmeier w,mckenzie se. prt-060318, a novel syk inhibitor, prevents heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model. blood.2011 feb 17;117(7):2241-6.
PRT-060318 Preparation Products And Raw materials
Raw materials
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