NX-5948 is an orally bioavailable, brain-penetrant Bruton’s tyrosine kinase (BTK) degrader. NX-5948 induces potent and selective degradation of both wild-type and mutant BTK (including C481S) in B cells, leading to downstream signaling inhibition. In vitro, it achieves complete BTK degradation at sub-nanomolar concentrations (DC₅₀ < 1 nM in Ramos cells), with sustained suppression of BCR signaling and downstream markers such as pPLCγ2 and pERK. In vivo, oral dosing in xenograft mouse models results in robust BTK degradation in peripheral blood and lymphoid tissues, and significant tumor growth inhibition in BTK-dependent lymphoma models. NX-5948 has demonstrated brain penetrance and BTK degradation in the CNS, supporting its evaluation in diseases with central nervous system involvement.
MedKoo Cat#: 125822
Name: NX-5948
CAS#: 2649400-34-8
Chemical Formula: C42H54N12O5
Exact Mass: 806.4300
Molecular Weight: 806.97
Elemental Analysis: C, 62.51; H, 6.75; N, 20.83; O, 9.91
The following data is based on the product molecular weight 806.97 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
