AZD-4320 is a BH3 mimetic and dual Bcl-2/Bcl-XL inhibitor with IC50 of <1 nM. AZD-4320 is an active metabolite of AZD-0466. AZD4320 has nanomolar affinity for Bcl-2 and Bcl-xL, and mechanistically drives cell death through the mitochondrial apoptotic pathway. AZD4320 demonstrates activity in both Bcl-2- and Bcl-xL-dependent hematologic cancer cell lines and enhanced activity in acute myeloid leukemia (AML) patient samples compared with the Bcl-2-selective agent venetoclax. A single intravenous bolus dose of AZD4320 induces tumor regression with transient thrombocytopenia, which recovers in less than a week, suggesting a clinical weekly schedule would enable targeting of Bcl-2/Bcl-xL-dependent tumors without incurring dose-limiting thrombocytopenia. AZD4320 demonstrates monotherapy activity in patient-derived AML and venetoclax-resistant xenograft models.
MedKoo Cat#: 206968
Name: AZD-4320
CAS#: 1357576-48-7 (free base)
Chemical Formula: C45H48ClF3N4O7S3
Exact Mass: 944.2326
Molecular Weight: 945.52
Elemental Analysis: C, 57.16; H, 5.12; Cl, 3.75; F, 6.03; N, 5.93; O, 11.84; S, 10.17
The following data is based on the product molecular weight 945.52 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 |
