TP-1287 is an orally bioavailable prodrug of Alvocidib (also known as Flavopiridol), designed to improve the pharmacokinetic limitations of the parent compound while retaining potent cyclin-dependent kinase 9 (CDK9) inhibition. Preclinical studies have shown that TP-1287 is rapidly converted to Alvocidib in vivo, resulting in sustained plasma levels of the active drug. Alvocidib inhibits CDK9 with low nanomolar IC₅₀ values (~3–5 nM) and blocks RNA polymerase II-mediated transcription, leading to downregulation of anti-apoptotic proteins like MCL-1 and induction of apoptosis in cancer cells. In xenograft models, oral TP-1287 demonstrated significant tumor growth inhibition and durable target engagement, with favorable safety and tolerability profiles compared to intravenous Alvocidib.
MedKoo Cat#: 462963
Name: TP1287
CAS#: 2044686-42-0
Chemical Formula: C21H21ClNO8P
Exact Mass: 481.0693
Molecular Weight: 481.82
Elemental Analysis: C, 52.35; H, 4.39; Cl, 7.36; N, 2.91; O, 26.56; P, 6.43
Early clinical studies (e.g., NCT03604783) have reported manageable toxicity and preliminary signs of antitumor activity in advanced solid tumors, supporting its continued development.
The following data is based on the product molecular weight 481.82 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 |
Early clinical studies (e.g., NCT03604783) have reported manageable toxicity and preliminary signs of antitumor activity in advanced solid tumors, supporting its continued development.
