| Identification | Back Directory | [Name]
4H-1-Benzopyran-4-one, 2-(2-chlorophenyl)-5-hydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]-7-(phosphonooxy)- | [CAS]
2044686-42-0 | [Synonyms]
TP1287
TP-1287
TP 1287
4H-1-Benzopyran-4-one, 2-(2-chlorophenyl)-5-hydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]-7-(phosphonooxy)- | [Molecular Formula]
C21H21ClNO8P | [MOL File]
2044686-42-0.mol | [Molecular Weight]
481.82 |
| Chemical Properties | Back Directory | [Boiling point ]
717.1±70.0 °C(Predicted) | [density ]
1.576±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
1.58±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
TP-1287, a prodrug of Alvocidib (HY-10005), is an orally active CDK9 inhibitor[1]. | [in vivo]
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]. | Animal Model: | RPMI-8226 xenograft model for multiple myeloma[1] | | Dosage: | 2.5, 7.5, and 15 mg/kg | | Administration: | Oral | | Result: | Achieved tumor growth inhibition (%TGI) of 56.0, 76.6, and 93.9% at doses of 2.5, 7.5, and 15 mg/kg, respectively. |
| [IC 50]
CDK9 | [References]
[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. |
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