Locnartecan, also known as PEN-866, Sdc-trap 0063, and STA 12-8666, is a heat shock protein 90 (HSP90) inhibitor-drug conjugates (HDC). STA-12-8666 is binds the tumor-concentrated active form of heat shock protein 90 (HSP90), with a cleavable linker attached to SN-38, the active metabolite of irinotecan. STA-12-8666 selectively binds activated HSP90 and releases its cytotoxic payload resulting in drug accumulation in pancreatic cancer cells in vivo. STA-12-8666 also demonstrated dramatically superior activity in comparison to equimolar doses of irinotecan against 5 patient-derived pancreatic adenocarcinoma xenografts with prolonged remissions in some tumors. Analysis of activity of STA-12-8666 against tumor tissues and matched cell lines demonstrated prolonged accumulation and release of cytotoxic payload in the tumor leading to DNA damage response and cell cycle arrest.
MedKoo Cat#: 593191
Name: Locnartecan
CAS#: 1472614-83-7 (free acid)
Chemical Formula: C49H49N7O9
Exact Mass: 879.3600
Molecular Weight: 879.97
Elemental Analysis: C, 66.88; H, 5.61; N, 11.14; O, 16.36
The following data is based on the product molecular weight 879.97 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 |
