ChemicalBook > CAS DataBase List > PRT-060318

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);P142-76|||PRT318|||PRT-060318 2HCl;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
CBNumber
CB12731127
Molecular Formula
C18H24N6O
Formula Weight
340.42
MOL File
1194961-19-7.mol
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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
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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.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2505
Product name
PRT-060318
Purity
≥95% (HPLC)
Packaging
5mg
Price
$123
Updated
2024/03/01
Sigma-Aldrich
Product number
SML2505
Product name
PRT-060318
Purity
≥95% (HPLC)
Packaging
25mg
Price
$347
Updated
2024/03/01
Cayman Chemical
Product number
22476
Product name
PRT060318
Purity
≥98%
Packaging
5mg
Price
$144
Updated
2024/03/01
Cayman Chemical
Product number
22476
Product name
PRT060318
Purity
≥98%
Packaging
10mg
Price
$274
Updated
2024/03/01
Cayman Chemical
Product number
22476
Product name
PRT060318
Purity
≥98%
Packaging
25mg
Price
$502
Updated
2024/03/01
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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

Preparation Products

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PRT-060318 Suppliers

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1194961-19-7, PRT-060318Related Search:


  • PRT-060318
  • PRT-060318(PRT318)
  • 2-[[(1R,2S)-2-Aminocyclohexyl]amino]-4-[(3-methylphenyl)amino]-5-pyrimidinecarboxamide
  • P 142-76
  • PRT 318
  • 2-(((1R,2S)-2-aminocyclohexyl)amino)-4-(m-tolylamino)pyrimidine-5-carboxamide
  • CS-1688
  • PRT-060318 ≥95%
  • PRT 060318 ;PRT060318;PRT 318;PRT-318;PRT318
  • 5-Pyrimidinecarboxamide, 2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[(3-methylphenyl)amino]-
  • 4-(3-methyl-phenyl-amino-)-2-(2-amino-cyclo-hexyl-amino-)-pyrimidine-5-carboxamide
  • P142-76|||PRT318|||PRT-060318 2HCl
  • 2-{[(1R,2S)-2-aminocyclohexyl]amino}-4-[(3-methylphenyl)amino]pyrimidine-5-carboxamide
  • 1194961-19-7
  • C18H27Cl3N6O