| Stereochemistry | ACHIRAL |
| Molecular Formula | C24H30ClN7O2S |
| Molecular Weight | 516.059 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)S(=O)(=O)C1=C(NC2=C(Cl)C=NC(NC3=CC=C(CN4CCN(C)CC4)C=C3)=N2)C=CC=C1
InChI
InChIKey=YUAALFPUEOYPNX-UHFFFAOYSA-N
InChI=1S/C24H30ClN7O2S/c1-30(2)35(33,34)22-7-5-4-6-21(22)28-23-20(25)16-26-24(29-23)27-19-10-8-18(9-11-19)17-32-14-12-31(3)13-15-32/h4-11,16H,12-15,17H2,1-3H3,(H2,26,27,28,29)
| Molecular Formula | C24H30ClN7O2S |
| Molecular Weight | 516.059 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
HCI-2084 (wider known as TP-0903) is developing by Tolero Pharmaceuticals for the treatment of different cancers. HCI-2084 is a small molecule AXL receptor tyrosine kinase (RTK) inhibitor. AXL is involved in maintaining a mesenchymal phenotype in cancer cells that enhanced cell survival in stressed environments, and increased resistance to targeted therapies compared to epithelial cells. AXL overexpression has been observed in multiple tumor types that have acquired resistance to various agents. TP-0903 is participating in phase I/II clinical trial in patients with previously treated chronic lymphocytic leukemia (CLL). This study will investigate the safety, pharmacokinetics, pharmacodynamics, and clinical activity of TP-0903. Besides, phase I is currently being conducted in patients with advanced solid tumors in the presence of TP-0903. In addition, TP-0903 was investigated in neuroblastoma (NB) cells, where this drug makes NB cells more vulnerable to the conventional chemotherapeutics.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 0.027 µM [IC50] | |||
| 3.0 nM [IC50] | |||
| 12.4 nM [IC50] | |||
PubMed
Sample Use Guides
Monotherapy: PHASE 1: TP-0903 (HCI-2084) will be a 25 mg flat dose. The study drug will be administered orally once daily for 28 days (each cycle is 28 days; no drug-free period). Patients may continue to receive TP-0903 in 28-day cycles at the same dose given during Cycle 1 until they experience unacceptable toxicity or unequivocal disease progression. No intrapatient escalation of the TP-0903 dose is permitted.
PHASE 2: The starting dose of TP-0903 will be the RP2D determined during Phase 1. TP 0903 will be administered orally at a fixed dose once daily for 28 days (each cycle is 28 days; no drug-free period) with repeated cycles permitted until a patient experiences unacceptable toxicity or unequivocal disease progression.
Route of Administration:
Oral
