SF1126
DRACPC ID DRACPC0016
Active Ingredients SF1126
Description A water soluble, small-molecule prodrug containing the pan-PI3K/mTOR inhibitor LY294002/SF1101 conjugated to the RGD-containing tetra-peptide SF1174 with potential antineoplastic and antiangiogenic activities. The targeting peptide SF1174 moiety of pan-PI3K/mTOR inhibitor SF1126 selectively binds to cell surface integrins and, upon cell entry, the agent is hydrolyzed to the active drug SF1101; SF1101 selectively inhibits all isoforms of phosphoinositide-3-kinase (PI3K) and other members of the PI3K superfamily, such as the mammalian target of rapamycin (mTOR) and DNA-PK. By inhibiting the PI3K signaling pathway, this agent may inhibit tumor cell and tumor endothelial cell proliferation and survival.
Synonyms pan-PI3K/mTOR Inhibitor SF1126; SF1126
Type Small Molecule
Disease Various forms of cancer
Classification
pan-PI3K/mTOR Inhibitor Peptide and derivative Peptide-Drug Conjugates Cancer Targeted Conjugates
Structure Information
Molecular Formula C39H48N8O14
Molecular Weight 852.8
Active Sequence XRGDS
Sequence Length 5
Modification X=LY294002 (Small-molecule prodrug containing the pan-PI3K/mTOR inhibitor)
IUPAC Name (3S)-4-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-3-[[2-[[(2S)-5-(diaminomethylideneamino)-2-[[4-oxo-4-[[4-(4-oxo-8-phenylchromen-2-yl)morpholin-4-ium-4-yl]methoxy]butanoyl]amino]pentanoyl]amino]acetyl]amino]-4-oxobutanoate
InChI InChI=1S/C39H48N8O14/c40-39(41)42-13-5-10-26(36(55)43-20-31(51)45-27(18-33(52)53)37(56)46-28(21-48)38(57)58)44-30(50)11-12-34(54)60-22-47(14-16-59-17-15-47)32-19-29(49)25-9-4-8-24(35(25)61-32)23-6-2-1-3-7-23/h1-4,6-9,19,26-28,48H,5,10-18,20-22H2,(H9-,40,41,42,43,44,45,46,50,51,52,53,55,56,57,58)/t26-,27-,28-/m0/s1
InChI_Key SVNJBEMPMKWDCO-KCHLEUMXSA-N
SMILES O=C([O-])C[C@H](NC(CNC([C@@H](NC(CCC(OC[N+]1(C2=CC(C3=C(O2)C(C4=CC=CC=C4)=CC=C3)=O)CCOCC1)=O)=O)CCC/N=C(N)\N)=O)=O)C(N[C@H](C(O)=O)CO)=O
External Codes
PubChem CID 92043140
DrugBank Accession Number DB05210
NCI Thesaurus Code C85469
UNII DL0Q912033 GSRS
CAS 936487-67-1
Drug approval
Drug indication
For the treatment of various forms of cancer.
The drug is not approved.
| ClinicalTrials.gov Identifier | Title | Condition or disease | Phase | Purpose |
|---|---|---|---|---|
| NCT03059147 | A Phase I Study of SF1126, a Dual PI3 Kinase and Bromodomain Inhibitor, in Combination With Nivolumab in Patients With Advanced or Metastatic Hepatocellular Carcinoma and Child-Pugh A-B7 Cirrhosis | Advanced Hepatocellular Carcinoma | Phase 1 | Treatment |
| NCT02337309 | Phase I Study of SF1126 for Patients With Relapsed or Refractory Neuroblastoma | Neuroblastoma | Phase 1 | Treatment |
| NCT02644122 | A Phase II Open Label Study of the PI3 Kinase (PI-3) Inhibitor, SF1126, in Patients With Recurrent or Progressive SCCHN and Mutations in PIK3CA Gene and/or PI-3 Kinase Pathway Genes | Metastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma | Phase 2 | Treatment |
| NCT00907205 | A Phase I Open Label Safety, Pharmacokinetic and Pharmacodynamic Dose Escalation Study of SF1126, A PI3 Kinase (PI3K) Inhibitor, Given Twice Weekly By IV Infusion To Patients With Advanced or Metastatic Tumors | Advanced or Metastatic Solid Tumors; Cancer; Solid Cancers | Phase 1 | Treatment |
More clinical information is obtained from ClinicalTrials.gov.
