| Stereochemistry | ACHIRAL |
| Molecular Formula | C22H14FN5 |
| Molecular Weight | 367.3785 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(C2=NC3=C(N2)C4=CC=CN=C4C5=C3C=CC=N5)C6=C(N1)C=CC(F)=C6
InChI
InChIKey=NIRXBXIPHUTNNI-UHFFFAOYSA-N
InChI=1S/C22H14FN5/c1-11-17(15-10-12(23)6-7-16(15)26-11)22-27-20-13-4-2-8-24-18(13)19-14(21(20)28-22)5-3-9-25-19/h2-10,26H,1H3,(H,27,28)
APTO-253 is a novel small molecule that can induce expression of the genes that code for the Krüppel-like factor 4 (KLF4) master transcription factor and for the p21 cell cycle inhibitor protein, and can inhibit expression of the c-Myc oncogene, leading to cell cycle arrest and programmed cell death (apoptosis) in human-derived solid tumor and hematologic cancer cells. A Phase 1 study with APTO-253 was completed and demonstrated modest clinical activity in patients with colon cancer, acute leukemia, myelodysplastic syndrome, hematological malignancies and non-small cell lung cancers.
Originator
Approval Year
Sourcing
PubMed
Patents
Sample Use Guides
APTO-253 HCl will be given in ascending doses starting from 20 mg/m2 until the maximum administered dose or appropriate dose is reached. Patients will be treated on APTO-253 HCl for at least 1 cycle (28 days) for safety evaluation.
Route of Administration:
Intravenous
APTO-253 showed potent antiproliferative activity in vitro against a panel of blood cancer cell lines, with ηM IC50 values in acute myelogenous leukemia (6.9 - 305 ηM), acute lymphoblastic leukemia and chronic myeloid leukemia (39 – 250 ηM), non-Hodgkin’s lymphoma (11 – 190 ηM) and multiple myeloma (72 – 180 ηM).
ACTIVE MOIETY
SALT/SOLVATE (PARENT)
