Description
A potent, small-molecule dual insulin-like growth factor-1 receptor (IGF-1R)/insulin receptor (IR) kinase inhibitor. Inhibits IGF-1R and IR kinases with IC₅₀ values of 35 nM and 75 nM, respectively. Linsitinib selectively blocks the autophosphorylation of both human IGF-1R and IR, inhibits the proliferation of a variety of tumor cell lines in vitro, and displays robust in vivo anti-tumor efficacy in an IGF-1R-driven xenograft model when administered orally.
Linsitinib is a potent, small-molecule dual insulin-like growth factor-1 receptor (IGF-1R)/insulin receptor (IR) kinase inhibitor. Inhibits IGF-1R and IR kinases with IC₅₀ values of 35 nM and 75 nM, respectively
2294 | Linsitinib, Free base DataSheet
Alternate Name/Synonyms: (1S,3S)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol; OSI-906; OSI 906AA
Appearance: White to off-white solid
Formulation: N/A
CAS Number: 867160-71-2
Structure Available?: Yes
Peptide sequence: No
Salt Form: No
Molecular Formula: C₂₆H₂₃N₅O
Molecular Weight: 421.49
Cell-Permeable?: Yes
Purity: ≥99% by HPLC
Solubilities: DMSO (~50 mg/ml) or Ethanol (~3 mg/ml)
Handling: Protect from air and light
Country of Origin: USA
Tag Line: A potent, dual insulin-like growth factor-1 receptor (IGF-1R)/insulin receptor (IR) kinase inhibitor.
MDL Number: MFCD12912153
PubChem CID: 11640390
SMILES: CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O
InChi: InChI=1S/C26H23N5O/c1-26(32)14-19(15-26)25-30-22(23-24(27)28-11-12-31
InChi Key: PKCDDUHJAFVJJB-UHFFFAOYSA-N
Additional Information
Storage Condition: |
-20 ̊C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |