Identification

Name
SF1126
Accession Number
DB05210
Type
Small Molecule
Groups
Investigational
Description

SF1126 is an integrin-targeted PI3 kinase inhibitor.

Synonyms
Not Available
Categories
UNII
Not Available
CAS number
Not Available
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

For the treatment of various forms of cancer.

Structured Indications
Not Available
Pharmacodynamics

SF1126 is a covalent conjugate of LY294002 that contains a peptide-based targeting group to help increase the localization of the drug in the neovascular component supporting tumor growth. SF1126 is a highly water soluble solid which aids its administration via i.v. or s.c. injections. In vivo it converts spontaneously at physiological pH to LY294002 in a way that is well tolerated in mice, rats, and dogs. SF1126 has been evaluated in numerous animal tumor models showing good tumor inhibition or tumor regression.

Mechanism of action

SF1126 is a small molecule conjugate containing a pan-PI3K inhibitor that selectively inhibits all PI3K class IA isoforms and other key members of the PI3K superfamily, including DNA-PK and mTOR. A major factor in tumor resistance to approved chemotherapy agents is thought to be the activation of the PI3K/PTEN pathway. As a result, it is thought that inhibiting this pathway, via SF1126, could cause the resetting of sensitivity to approved agents and exhibit synergistic anticancer effects.

TargetActionsOrganism
UPhosphatidylinositol 3-kinase regulatory subunit alphaNot AvailableHuman
UPhosphatidylinositol 3-kinase regulatory subunit betaNot AvailableHuman
UPhosphatidylinositol 3-kinase regulatory subunit gammaNot AvailableHuman
UDNA-dependent protein kinase catalytic subunitNot AvailableHuman
USerine/threonine-protein kinase mTORNot AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

References

General References
Not Available
External Links
PubChem Substance
347910028

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentAdvanced or Metastatic Solid Tumors / Cancers / Solid Cancers1
1RecruitingTreatmentAdvanced Hepatocellular Carcinoma1
1RecruitingTreatmentNeuroblastomas1
2TerminatedTreatmentMetastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Transmembrane receptor protein tyrosine kinase adaptor activity
Specific Function
Binds to activated (phosphorylated) protein-Tyr kinases, through its SH2 domain, and acts as an adapter, mediating the association of the p110 catalytic unit to the plasma membrane. Necessary for t...
Gene Name
PIK3R1
Uniprot ID
P27986
Uniprot Name
Phosphatidylinositol 3-kinase regulatory subunit alpha
Molecular Weight
83597.675 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Receptor tyrosine kinase binding
Specific Function
Regulatory subunit of phosphoinositide-3-kinase (PI3K), a kinase that phosphorylates PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3...
Gene Name
PIK3R2
Uniprot ID
O00459
Uniprot Name
Phosphatidylinositol 3-kinase regulatory subunit beta
Molecular Weight
81544.505 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
1-phosphatidylinositol-3-kinase regulator activity
Specific Function
Binds to activated (phosphorylated) protein-tyrosine kinases through its SH2 domain and regulates their kinase activity. During insulin stimulation, it also binds to IRS-1.
Gene Name
PIK3R3
Uniprot ID
Q92569
Uniprot Name
Phosphatidylinositol 3-kinase regulatory subunit gamma
Molecular Weight
54448.0 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Transcription factor binding
Specific Function
Serine/threonine-protein kinase that acts as a molecular sensor for DNA damage. Involved in DNA non-homologous end joining (NHEJ) required for double-strand break (DSB) repair and V(D)J recombinati...
Gene Name
PRKDC
Uniprot ID
P78527
Uniprot Name
DNA-dependent protein kinase catalytic subunit
Molecular Weight
469084.155 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Tfiiic-class transcription factor binding
Specific Function
Serine/threonine protein kinase which is a central regulator of cellular metabolism, growth and survival in response to hormones, growth factors, nutrients, energy and stress signals. MTOR directly...
Gene Name
MTOR
Uniprot ID
P42345
Uniprot Name
Serine/threonine-protein kinase mTOR
Molecular Weight
288889.05 Da

Drug created on October 21, 2007 16:24 / Updated on November 06, 2017 06:45