Ruserontinib
drugOn this page
Also known as Sklb 1028SKLB-1028Sklb1028
Summary
Ruserontinib (CHEMBL3678958) is a phase-3 clinical-stage small molecule targeting FLT3; indicated across 2 conditions including acute myeloid leukemia and neoplasm.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 1 (FLT3)
- Indications: 2 conditions
- Clinical trials: 7
- Chemistry: 443.5 Da · C24H29N9
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL3678958 |
| Name | Ruserontinib |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 54760385 |
| Molecular formula | C24H29N9 |
| Molecular weight | 443.5 |
| InChIKey | WSOHOUHPUOAXIN-UHFFFAOYSA-N |
SMILES: CC(C)N1C2=NC(=NC=C2N=C1NC3=CN=CC=C3)NC4=CC=C(C=C4)N5CCN(CC5)C
IUPAC name: 2-N-[4-(4-methylpiperazin-1-yl)phenyl]-9-propan-2-yl-8-N-pyridin-3-ylpurine-2,8-diamine
Also known as: Ruserontinib, Sklb 1028, SKLB-1028, Sklb1028, RUSERONTINIB
Patent coverage: 63 distinct patent families (149 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 138 (93%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| FLT3 | fms related receptor tyrosine kinase 3 | Inhibition | 7.26 | 0.9% | P36888 |
Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Epidermal growth factor receptor.
Bioactivity
ChEMBL activities: 3 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| EGFR | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_17698867 |
| EGFR | 7.51 | IC50 | 31 | nM | CHEMBL_ACT_16329229 |
| EGFR | 7.19 | IC50 | 64 | nM | CHEMBL_ACT_17698894 |
Target pathways
Aggregated over 1 target gene(s): FLT3.
Top Reactome pathways
27 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| PI3K Cascade | 1 | FLT3 |
| PIP3 activates AKT signaling | 1 | FLT3 |
| Constitutive Signaling by Aberrant PI3K in Cancer | 1 | FLT3 |
| RAF/MAP kinase cascade | 1 | FLT3 |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 1 | FLT3 |
| FLT3 Signaling | 1 | FLT3 |
| STAT5 Activation | 1 | FLT3 |
| FLT3 mutants bind TKIs | 1 | FLT3 |
| STAT5 activation downstream of FLT3 ITD mutants | 1 | FLT3 |
| KW2449-resistant FLT3 mutants | 1 | FLT3 |
| semaxanib-resistant FLT3 mutants | 1 | FLT3 |
| crenolanib-resistant FLT3 mutants | 1 | FLT3 |
| gilteritinib-resistant FLT3 mutants | 1 | FLT3 |
| lestaurtinib-resistant FLT3 mutants | 1 | FLT3 |
| midostaurin-resistant FLT3 mutants | 1 | FLT3 |
| pexidartinib-resistant FLT3 mutants | 1 | FLT3 |
| ponatinib-resistant FLT3 mutants | 1 | FLT3 |
| quizartinib-resistant FLT3 mutants | 1 | FLT3 |
| sorafenib-resistant FLT3 mutants | 1 | FLT3 |
| sunitinib-resistant FLT3 mutants | 1 | FLT3 |
| tandutinib-resistant FLT3 mutants | 1 | FLT3 |
| linifanib-resistant FLT3 mutants | 1 | FLT3 |
| tamatinib-resistant FLT3 mutants | 1 | FLT3 |
| Signaling by FLT3 ITD and TKD mutants | 1 | FLT3 |
| Negative regulation of FLT3 | 1 | FLT3 |
| FLT3 signaling through SRC family kinases | 1 | FLT3 |
| FLT3 signaling by CBL mutants | 1 | FLT3 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| leukocyte homeostasis | 1 |
| myeloid progenitor cell differentiation | 1 |
| pro-B cell differentiation | 1 |
| cell surface receptor protein tyrosine kinase signaling pathway | 1 |
| positive regulation of cell population proliferation | 1 |
| cell migration | 1 |
| peptidyl-tyrosine phosphorylation | 1 |
| cytokine-mediated signaling pathway | 1 |
| hemopoiesis | 1 |
| B cell differentiation | 1 |
| common myeloid progenitor cell proliferation | 1 |
| positive regulation of tyrosine phosphorylation of STAT protein | 1 |
| regulation of apoptotic process | 1 |
| positive regulation of MAP kinase activity | 1 |
| positive regulation of MAPK cascade | 1 |
Indications & clinical
Indications
2 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| acute myeloid leukemia | 3 | MONDO:0018874 | EFO:0000222 |
| neoplasm | 2 | MONDO:0005070 | EFO:0000616 |
Clinical trials
Total trials: 7.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 6 |
| PHASE3 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT04716114 | PHASE3 | UNKNOWN | A Study of SKLB1028 Versus Salvage Chemotherapy in Patients With Relapsed or Refractory (R/R) AML With FLT3-Mutated |
| NCT02859948 | PHASE1 | UNKNOWN | A Study of SKLB1028 in Subjects With Relapsed/Refractory Acute Myeloid Leukemia |
| NCT05069870 | PHASE1 | UNKNOWN | A Study to Investigate the Drug-drug Interactions (DDIs) of SKLB1028 With Itraconazole, Gemfibrozil or Rifampicin in Healthy Subjects |
| NCT05070195 | PHASE1 | COMPLETED | A Study to Investigate the Drug-drug Interactions (DDIs) Between SKLB1028 and Midazolam in Healthy Subjects |
| NCT05072522 | PHASE1 | UNKNOWN | A Study of SKLB1028 in Patients With Advanced Solid Tumor |
| NCT05109663 | PHASE1 | COMPLETED | A Dose Escalation and Food Effect Study of SKLB1028 in Healthy Subjects |
| NCT05369858 | PHASE1 | COMPLETED | A Mass Balance and Biotransformation Study of [14C]SKLB1028 in Chinese Healthy Male Subjects |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
116 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| AFATINIB | ChEMBL + PubChem | Phase 4 (approved) | FLT3 |
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | FLT3 |
| FOSTAMATINIB | ChEMBL + PubChem | Phase 4 (approved) | FLT3 |
| PAZOPANIB | ChEMBL + PubChem | Phase 4 (approved) | FLT3 |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | FLT3 |
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | FLT3 |
| AXITINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| CERITINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| DASATINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| FILGOTINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| GEFITINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| GILTERITINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| IBRUTINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| IMATINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | FLT3 |
| NERATINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| NILOTINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | FLT3 |
| PACRITINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| PALBOCICLIB | ChEMBL | Phase 4 (approved) | FLT3 |
| PEXIDARTINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| PONATINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| PRALSETINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| QUIZARTINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| SORAFENIB | ChEMBL | Phase 4 (approved) | FLT3 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | FLT3 |
| TIVOZANIB | ChEMBL | Phase 4 (approved) | FLT3 |
| VANDETANIB | ChEMBL | Phase 4 (approved) | FLT3 |
| ALVOCIDIB | ChEMBL | Phase 3 | FLT3 |
| BARASERTIB | ChEMBL | Phase 3 | FLT3 |
| CANERTINIB | ChEMBL | Phase 3 | FLT3 |
| CEDIRANIB | ChEMBL | Phase 3 | FLT3 |
| CRENOLANIB | ChEMBL | Phase 3 | FLT3 |
| DEFACTINIB | ChEMBL | Phase 3 | FLT3 |
| DOVITINIB | ChEMBL | Phase 3 | FLT3 |
| ENTOSPLETINIB | ChEMBL | Phase 3 | FLT3 |
| ENZASTAURIN | ChEMBL | Phase 3 | FLT3 |
| LEROCICLIB | ChEMBL | Phase 3 | FLT3 |
| LESTAURTINIB | ChEMBL | Phase 3 | FLT3 |
| LINIFANIB | ChEMBL | Phase 3 | FLT3 |
| LINSITINIB | ChEMBL | Phase 3 | FLT3 |
| MOTESANIB | ChEMBL | Phase 3 | FLT3 |
| OLVEREMBATINIB | ChEMBL | Phase 3 | FLT3 |
| ORANTINIB | ChEMBL | Phase 3 | FLT3 |
| QUERCETIN | ChEMBL | Phase 3 | FLT3 |
| RESVERATROL | ChEMBL | Phase 3 | FLT3 |
| RUBOXISTAURIN | ChEMBL | Phase 3 | FLT3 |
| SARACATINIB | ChEMBL | Phase 3 | FLT3 |
| SEMAXANIB | ChEMBL | Phase 3 | FLT3 |
| SITRAVATINIB | ChEMBL | Phase 3 | FLT3 |
| SURUFATINIB | ChEMBL | Phase 3 | FLT3 |
| VIMSELTINIB | ChEMBL | Phase 3 | FLT3 |
| AKN-028 | ChEMBL | Phase 2 | FLT3 |
Related Atlas pages
- Genes: FLT3
- Diseases: acute myeloid leukemia
- Drugs: Afatinib, Crizotinib, Fostamatinib, Pazopanib, Regorafenib, Abemaciclib, Axitinib, Bosutinib, Brigatinib, Cabozantinib, Ceritinib, Dasatinib, Entrectinib, Erlotinib, Fedratinib, Filgotinib, Gefitinib, Gilteritinib, Ibrutinib, Imatinib, Infigratinib, Midostaurin, Neratinib, Nilotinib, Nintedanib, Pacritinib, Palbociclib, Pexidartinib, Ponatinib, Pralsetinib, Quizartinib, Sorafenib, Sunitinib, Tivozanib, Vandetanib, Alvocidib, Barasertib, Canertinib, Cediranib, Crenolanib, Defactinib, Dovitinib, Entospletinib, Enzastaurin, Lerociclib, Lestaurtinib, Linifanib, Linsitinib, Motesanib, Olverembatinib, Orantinib, Quercetin, Resveratrol, Ruboxistaurin, Saracatinib, Semaxanib, Sitravatinib, Surufatinib, Vimseltinib