All AbMole products are for research use only, cannot be used for human consumption.
Pirtobrutinib (LOXO-305, LY 3527727, RXC-005) is a first-in-class, highly selective, non-covalent BTK inhibitor that inhibits multiple BTK C481 substitution mutations. Pirtobrutinib is more than 300-fold selective for BTK compared to 370 other kinases.Pirtobrutinib inhibits both wild-type BTK and BTK C481S-mediated kinase activity with nanomolar potency.Pirtobrutinib inhibits autophosphorylation of WT BTK (Y223) with an IC50 of 3.68 nM. Pirtobrutinib inhibited the autophosphorylation of WT BTK (Y223) with an IC50 of 3.68 nM. Pirtobrutinib inhibited the autophosphorylation of BTK C481S Y223, C481T Y223, and C481R Y223, with IC50s of 8.45, 7.23, and 11.73 nM, respectively.
| Cell Experiment | |
|---|---|
| Cell lines | MEC-1 WT, MEC-1-IR and MEC-1-AR cells |
| Preparation method | Subsequently, the media were aspirated, and fresh media containing the specified concentrations of pirtobrutinib, CAL101, or MK2206—namely, 0.05, 0.5, and 5 μM—were gently added to the respective wells. |
| Concentrations | 0.05, 0.5, and 5 μM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | Immunodeficiency mice |
| Formulation | DMSO |
| Dosages | 50 mg/kg |
| Administration | Oral gavage |
| Molecular Weight | 479.43 |
| Formula | C22H21F4N5O3 |
| CAS Number | 2101700-15-4 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage | 2-8°C, sealed |
[2] Diana Romero. Nat Rev Clin Oncol. Initial pirtobrutinib data show promise
| Related BTK Products |
|---|
| PCI-32765
PCI-32765 (Ibrutinib) is a potent, selective and orally bioavailable irreversible inhibitor of BTK with IC50 value of 0.46 nM. |
| Spebrutinib (AVL-292)
Spebrutinib (AVL-292) is an oral, potent and selective small molecule covalent inhibitor of Btk (IC50 < 0.5 nM). |
| CNX-774
CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM. |
| GDC-0834
GDC-0834 is a novel potent and selective BTK inhibitor with IC50 of 5.9 nM. |
| CGI1746
CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
