1575596-29-0
1575596-29-0 structure
- Name: PRN 1008
- Chemical Name: PRN1008
- CAS Number: 1575596-29-0
- Molecular Formula: C36H40FN9O3
- Molecular Weight: 665.76
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Btk
- Create Date: 2019-01-20 05:47:05
- Modify Date: 2024-01-13 23:10:18
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PRN1008 is a reversible covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
| Name | PRN1008 |
|---|
| Description | PRN1008 is a reversible covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM. |
|---|---|
| Related Catalog | |
| Target |
BTK:1.3 nM (IC50) BMX:1.0 nM (IC50) ITK:440 nM (IC50) TEC:0.8 nM (IC50) RLK:1.2 nM (IC50) BLK:6.3 nM (IC50) EGFR:520 nM (IC50) ERBB2:3900 nM (IC50) ERBB4:11.3 nM (IC50) |
| In Vitro | PRN1008 is a reversible covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3±0.5 nM. PRN1008 is also found to be highly selectively when tested in a panel of 251 other kinases. Cysteine targeting of BTK by PRN1008 results in a slow off-rate demonstrated by retention of 79±2% of binding to BTK in PBMC 18 hours after washing away the compound in vitro. The covalent cysteine binding is completely reversible after denaturation of the target. Anti-IgM induces human B cell proliferation (10% serum) and B cell CD69 expression are inhibited by PRN1008 with IC50 of 5±2.4 nM and 123±38 nM, respectively[2]. |
| In Vivo | In vivo PRN1008 demonstrates enduring pharmacodynamic effects after the compound has cleared from circulation, consistent with extended target residence time. PRN1008 also reverses and completely suppresses collagen-induced arthritis in rats in a dose dependent manner which allows correlation of target occupancy and disease modification[2]. |
| References |
| Molecular Formula | C36H40FN9O3 |
|---|---|
| Molecular Weight | 665.76 |
| Storage condition | 2-8℃ |