Sonrotoclax, also known as BGB-11417, is a potent BCL2 inhibitor (IC50 WT biochemical = 0.019 nM). BGB-11417 exhibits strong in vitro and in vivo inhibitory activity against both WT Bcl-2 and the G101V mutant, as well as excellent selectivity over Bcl-xL without obvious cytochrome P450 inhibition. Sonrotoclax showed 7−63-fold more potent than the other clinical Bcl-2 inhibitors, which was consistent with the 8−21-fold greater potency in the RS4;11 cell viability assay. Sonrotoclax exhibited 16−168-fold more potent in the Bcl-2 G101V mutant biochemical assay and 16−27-fold more potent in Bcl-2 G101V knock-in the RS4; cell viability assay than the other clinical Bcl-2 inhibitors. Sonrotoclax showed remarkably better PD and efficacy than venetoclax in DLBCL (Toledo) xenograft models and RS4; Bcl-2 G101V xenograft models. Sonrotoclax is highly effective in treating hematological cancers, including certain indications of NHL, and potentially overcomes the Bcl.
MedKoo Cat#: 130056
Name: Sonrotoclax
CAS#: 2383086-06-2
Chemical Formula: C49H59N7O7S
Exact Mass: 889.4197
Molecular Weight: 890.11
Elemental Analysis: C, 66.12; H, 6.68; N, 11.02; O, 12.58; S, 3.60
The following data is based on the product molecular weight 890.11 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 |
