| Name | Pirtobrutinib |
| Description | Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 μM, Pirtobrutinib demonstrates no significant inhibition of non-kinase off-targets. |
| In vitro | Pirtobrutinib potently inhibits both wild-type BTK and BTK C481S-mediated kinase activity with nanomolar potency. Pirtobrutinib strongly inhibits WT BTK (Y223) autophosphorylation with an IC50 of 3.68 nM. Pirtobrutinib inhibits BTK C481S Y223, C481T Y223, and C481R Y223 autophosphorylation with IC50s of 8.45, 7.23, and 11.73 nM, respectively[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (114.72 mM), Sonication is recommended.
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| Keywords | LOXO 305 | inhibit | LOXO-305 | Btk | Pirtobrutinib | C81S | LOXO305 | Bruton tyrosine kinase | proliferative | Inhibitor | mutations | autophosphorylation |
| Inhibitors Related | evobrutinib | (±)-Zanubrutinib | CP-547632 | BMS-986142 | Edralbrutinib | Sunvozertinib | Ibrutinib | IBT6A | Orelabrutinib | Atuzabrutinib | Remibrutinib | CGI-1746 |
| Related Compound Libraries | Highly Selective Inhibitor Library | EMA Approved Drug Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
