Tiancimycin A is a potent enediyne natural product with exceptional cytotoxicity, primarily through DNA double-strand breaks mediated by a Bergman cyclization-derived diradical species. It exhibits sub-nanomolar antiproliferative activity against multiple human cancer cell lines, including IC₅₀ values of 0.13 nM (NCI-H460), 0.24 nM (HT-29), and 0.36 nM (MDA-MB-468). In vivo, Tiancimycin A demonstrated strong antitumor efficacy in xenograft models; for example, in an NCI-H460 lung cancer mouse model, a single dose of 0.25 mg/kg significantly suppressed tumor growth without overt toxicity. Its mechanism of action, narrow therapeutic window, and potent activity place it among the most promising enediyne analogs for use in antibody-drug conjugates (ADCs), where controlled delivery mitigates its systemic toxicity
MedKoo Cat#: 465445
Name: Tiancimycin A
CAS#: 1965327-09-6
Chemical Formula: C27H19NO8
Exact Mass: 485.1111
Molecular Weight: 485.45
Elemental Analysis: C, 66.80; H, 3.95; N, 2.89; O, 26.37
The following data is based on the product molecular weight 485.45 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 |
