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Linsitinib

Linsitinib Suppliers list
Company Name: Capot Chemical Co.,Ltd.
Tel: 571-85586718 +8613336195806
Email: sales@capotchem.com
Products Intro: Product Name:Cis-3-[8-Amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutanol
CAS:867160-71-2
Purity:98%(Min,HPLC) Package:100g;1kg;5kg,10kg,25kg,50kg
Company Name: Hangzhou FandaChem Co.,Ltd.
Tel: 008657128800458; +8615858145714
Email: fandachem@gmail.com
Products Intro: Product Name:Linsitinib
CAS:867160-71-2
Purity:As coa Package:As request Remarks:867160-71-2
Company Name: ATK CHEMICAL COMPANY LIMITED
Tel: +undefined-21-51877795
Email: ivan@atkchemical.com
Products Intro: Product Name:OSI-906 (Linsitinib)
CAS:867160-71-2
Purity:98% HPLC Package:5MG;10MG;50MG;100MG,1G,5G
Company Name: Biochempartner
Tel: 0086-13720134139
Email: candy@biochempartner.com
Products Intro: Product Name:Linsitinib
CAS:867160-71-2
Purity:98% HPLC LCMS Package:10G;20G
Company Name: Changzhou PBpharmaceutical R&D Co.,Ltd
Tel: 0519-83990708
Email: info@pbpharm.com
Products Intro: Product Name:OSI-906 (Linsitinib)
CAS:867160-71-2
Purity:98%+ Package:100MG-100KG Remarks:in stock or customized product

Linsitinib manufacturers

  • Linsitinib
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  • $0.00 / 1KG
  • 2022-10-14
  • CAS:867160-71-2
  • Min. Order: 1KG
  • Purity: 98%
  • Supply Ability: 1Ton
  • Linsitinib
  • Linsitinib pictures
  • $6.68 / 1KG
  • 2020-01-09
  • CAS:867160-71-2
  • Min. Order: 1KG
  • Purity: 97%-99%
  • Supply Ability: 1kg-1000kg

Related articles

  • Pharmacology of Linsitinib
  • Linsitinib is an experimental drug candidate for the treatment of various types of cancer. It is an inhibitor of the insulin r....
  • Oct 15,2019
Linsitinib Basic information
Description In vitro In vivo
Product Name:Linsitinib
Synonyms:cis-3-[8-Amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutanol;Linsitinib;OSI-906 Linsitinib;Cyclobutanol, 3-[8-aMino-1-(2-phenyl-7-quinolinyl)iMidazo[1,5-a]pyrazin-3-yl]-1-Methyl-, cis-;OSI 906AA;(1S,3r)-3-((S)-8-aMino-1-(2-phenylquinolin-7-yl)-2,3-dihydroiMidazo[1,5-a]pyrazin-3-yl)-1-Methylcyclobutanol;(1s,3r)-3-[4-aMino-3-(2-phenylquinolin-7-yl)iMidazo[1,5-a]pyrazin-1-yl]-1-Methylcyclobutan-1-ol;Linsitinib, Free Base
CAS:867160-71-2
MF:C26H23N5O
MW:421.49
EINECS:1533716-785-6
Product Categories:Tyrosine Kinase Inhibitors;Inhibitors;Amines;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals
Mol File:867160-71-2.mol
Linsitinib Structure
Linsitinib Chemical Properties
Melting point >175°C (dec.)
density 1.39
storage temp. -20°C
solubility Soluble in DMSO (up to 30 mg/ml)
form solid
pka14.84±0.40(Predicted)
color Yellow
Stability:Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Safety Information
MSDS Information
Linsitinib Usage And Synthesis
DescriptionLinsitinib (OSI-906) is a selective inhibitor of IGF-1R with IC50 of 35 nM in cell-free assays; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3.
In vitroOSI-906 inhibits IGF-1R autophosphorylation and activation of the downstream signaling proteins Akt, ERK1/2 and S6 kinase with IC50 of 0.028 to 0.13 μM. OSI-906 enables an intermediate conformation of the target protein through interactions with the C-helix. OSI-906 displays favorable metabolic stability in liver microsomes. OSI-906 fully inhibits both IR and IGF-1R phosphorylation at a concentration of 1 μM. OSI-906 inhibits proliferation of several tumor cell lines including non-small-cell lung cancer and colorectal cancer (CRC) tumor cell line with EC50 of 0.021 to 0.810 μM.
In vivoOSI-906 inhibits tumor growth in an IGF-1R-driven xenograft mouse model, with 100% TGI and 55% regression at a dose of 75 mg/kg and 60% TGI and no regression at a dose of 25 mg/kg. OSI-906 administration induces different elimination half-lives of itself in dog, rat and mice, the elimination half-lives are 1.18 hours, 2.64 hours and 2.14 hours, respectively. OSI-906 administration at different single dose once-daily in femal Sprague-Dawley rat and femal CD-1 mouse reveal that the Vmax is not dose-proportional to OSI-906 dose. OSI-906 elevates the blood glucose levels at a dose of 25 mg/kg after 12 days administration. OSI-906 administration at a single dose of 75 mg/kg in IGF-1R-driven full-length human IGF-1R (LISN) xenograft mouse model achieve maximal inhibition of IGF-1R phosphorylation (80%) between 4 and 24 hours with plasma drug concentrations of 26.6-4.77 μM. OSI-906 administered as a single dose of at 60 mg/kg in NCI-H292 xenografts mice inhibits uptake of glucose at 2, 4, and 24 hours post-treatment in vivo. OSI-906 inhibits the growth of tumors in NCI-H292 xenograft mouse model.
DescriptionThe binding of insulin-like growth factor 1 (IGF-1) to the IGF-1 receptor (IGF-1R) promotes cell growth while inhibiting apoptotic pathways. Overexpression of IGF-1R is found in certain solid tumors and hematologic neoplasias. However, insulin receptor (InsR) signaling can compensate for IGF-1R inhibition. Linsitinib is a dual inhibitor of IGF-1R and InsR kinases (IC50s = 35 and 75 nM, respectively). It also inhibits InsR-related receptor (IC50 = 75 nM) but is without effect (IC50 > 10 μM) against a large panel of other kinases. Linsitinib inhibits proliferation of a variety of tumor cell lines in vitro and has antitumor efficacy in an IGF-1R-driven xenograft mouse model when administered orally. A rapid, non-invasive method to predict the pharmacodynamic response to linsitinib has been reported.
UsesLinsitinib is a small-molecule dual insulin-like growth factor-1 receptor (IGF-IR) and insulin receptor (IR) kinase inhibitor. IGF-I receptor (IGF-IR) has been implicated in the promotion of tumorigenesis, metastasis and resistance to cancer therapies and thus Linsitinib may be a useful anticancer agent. Potent IGF-1R inhibitor.
DefinitionChEBI: 3-[8-amino-1-(2-phenyl-7-quinolinyl)-3-imidazo[1,5-a]pyrazinyl]-1-methyl-1-cyclobutanol is a member of quinolines and a member of cyclobutanes.
targetIGF-1R
storageStore at -20°C
References1) Mulvihill?et al.?(2009),?Discovery of OSI-906: a selective and orally efficacious inhibitor of the IGF-1 receptor and insulin receptor; Future Med. Chem.?1?1153 2) Bendell?et al.?(2015),?A phase Ib study of linsitinib (OSI-906), a dual inhibitor of IGF-1R and IR tyrosine kinase, in combination with everolimus as treatment for patients with refractory metastatic colorectal cancer; Invest. New Drugs?33?187 3) Pivonello?et al.?(2016),?The dual targeting of insulin and insulin-like growth factor 1 receptor enhances the mTOR inhibitor-mediated antitumor efficacy in hepatocellular carcinoma?; Oncotarget?7?9718 4) Lee?et al.?(2016),?Inhibition of IGF1R signaling abrogates resistance to afatinib (BIBW2992) in EGFR T790M mutant lung cancer cells; Mol. Carcinog.?55?991 5) Macaulay?et al.?(2016),?Phase I Dose-Escalation Study of Linsitinib (OSI-906) and Erlotinib in Patients with Advanced Solid Tumors; Clin. Cancer Res.?22?2897 6) De Lint?et al.?(2016),?Sensitizing Triple-Negative Breast Cancer to PI3K Inhibition by Cotargeting IGF1R; Mol. Cancer Ther.?15?1545
Linsitinib Preparation Products And Raw materials
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