For research use only. Not for therapeutic Use.
TP-1287, a prodrug of Alvocidib (HY-10005), is an orally active CDK9 inhibitor[1].
TP-1287 suppresses MCL-1 expression via CDK9-mediated regulation of RNA polymerase II[1].
TP-1287 (2.5-15 mg/kg; oral) suppresses tumor growth in models of multiple myeloma[1].
TP-1287 is highly soluble over a broader pH range than Alvocidib (HY-10005) and is efficiently metabolized to the parent compound in vivo, following oral administration[2].
| Catalog Number | I037425 |
| CAS Number | 2044686-42-0 |
| Synonyms | [2-(2-chlorophenyl)-5-hydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]-4-oxochromen-7-yl] dihydrogen phosphate |
| Molecular Formula | C21H21ClNO8P |
| Purity | ≥95% |
| InChI | InChI=1S/C21H21ClNO8P/c1-23-7-6-12(16(26)10-23)19-18(31-32(27,28)29)9-15(25)20-14(24)8-17(30-21(19)20)11-4-2-3-5-13(11)22/h2-5,8-9,12,16,25-26H,6-7,10H2,1H3,(H2,27,28,29)/t12-,16+/m0/s1 |
| InChIKey | YRNFLVUMZIRYKY-BLLLJJGKSA-N |
| SMILES | CN1CCC(C(C1)O)C2=C(C=C(C3=C2OC(=CC3=O)C4=CC=CC=C4Cl)O)OP(=O)(O)O |
| Reference | [1]. Tyagi E, et al. The Oral CDK9 Inhibitor, TP-1287, Is Active in Non-Clinical Models of Multiple Myeloma. Blood, 2018, 132: 3269. [2]. Kim W, et al. TP-1287, an oral prodrug of the cyclin-dependent kinase-9 inhibitor alvocidib. Cancer Research, 2017, 77(13_Supplement): 5133-5133. |
