1194961-19-7
1194961-19-7 structure
- Name: PRT-060318
- Chemical Name: prt-060318
- CAS Number: 1194961-19-7
- Molecular Formula: C18H24N6O
- Molecular Weight: 340.423
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Syk
- Create Date: 2016-01-17 22:10:10
- Modify Date: 2024-01-01 20:07:03
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PRT-060318 (PRT318) is a novel selective inhibitor of the tyrosine kinase Syk with an IC50 of 4 nM.
| Name | prt-060318 |
|---|---|
| Synonyms |
2-{[(1R,2S)-2-Aminocyclohexyl]amino}-4-[(3-methylphenyl)amino]-5-pyrimidinecarboxamide
PRT318 2-(((1R,2S)-2-aminocyclohexyl)amino)-4-(m-tolylamino)pyrimidine-5-carboxamide P142–76 5-Pyrimidinecarboxamide, 2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[(3-methylphenyl)amino]- PRT 060318 |
| Description | PRT-060318 (PRT318) is a novel selective inhibitor of the tyrosine kinase Syk with an IC50 of 4 nM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 4 nM (Syk)[1] |
| In Vitro | PRT318 is a potent inhibitor of purified Syk kinase with an IC50 of 4 nM. Syk kinase is inhibited by 92%, whereas all other kinases retains more than 70% at a concentration of 50 nM of PRT318[1]. PRT318 and P505-15 effectively antagonize CLL cell survival after B-cell receptor (BCR) triggering and in nurse-like cell-co-cultures. They inhibit BCR-dependent secretion of the chemokines CCL3 and CCL4 by CLL cells, and leukemia cell migration toward the tissue homing chemokines CXCL12, CXCL13, and beneath stromal cells. PRT318 and P505-15 inhibit Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering[2]. |
| In Vivo | PRT318 completely inhibits HIT immune complex-induced aggregation of both human and transgenic HIT mouse platelets. Pretreatment of mice with PRT318 markedly reduces HIT IC-induced thrombosis in the lungs. The Thrombosis Score is significantly lower for PRT318-treated mice compared with control[1]. |
| Cell Assay | PRT318 is dissolved in DMSO. Cells are incubated for 14 days in 24-well plates. CLL cells are cultured under standardized conditions on NLC or in suspension, in the presence or absence of PRT318 and P505-15. At 24, 48, 72 h, CLL cells are collected and assayed for cell viability[2]. |
| Animal Admin | Mice: Heparin-induced thrombocytopenia (HIT) model mice are treated with KKO (20 mg/kg body weight, intraperitoneally) on day 0. The mice are divided into sex- and weight-matched experimental and control groups. On days 1 to 7, experimental mice (n=6) receives PRT318 (30 mg/kg body weight) orally via gavage twice a day, whereas control mice (n=6) receives vehicle only (sterile water). Both groups receives heparin (1600 U/kg body weight, subcutaneously) once daily. Mice are anesthetized by isoflurane inhalation for injections and blood collections[1]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 602.1±65.0 °C at 760 mmHg |
| Molecular Formula | C18H24N6O |
| Molecular Weight | 340.423 |
| Flash Point | 317.9±34.3 °C |
| Exact Mass | 340.201172 |
| PSA | 118.95000 |
| LogP | 1.62 |
| Vapour Pressure | 0.0±1.7 mmHg at 25°C |
| Index of Refraction | 1.672 |