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Linsitinib

Linsitinib Structure
Linsitinib structure
CAS No.
867160-71-2
Chemical Name:
Linsitinib
Synonyms
OSI-906;CS-190;OSI 906AA;Linsitinib;OSI 906;OSI906;Linsitinib(OSI906);OSI-906 Linsitinib;Linsitinib USP/EP/BP;Linsitinib, Free Base;LINSITINIB;OSI 906; OSI906
CBNumber:
CB62501004
Molecular Formula:
C26H23N5O
Molecular Weight:
421.49
MDL Number:
MFCD12912153
MOL File:
867160-71-2.mol
MSDS File:
SDS
Last updated:2023-06-30 15:45:59
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Linsitinib Properties

Melting point >175°C (dec.)
Density 1.39
storage temp. -20°C
solubility Soluble in DMSO (up to 30 mg/ml)
form solid
pka 14.84±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.
NCI Dictionary of Cancer Terms OSI-906
FDA UNII 15A52GPT8T
NCI Drug Dictionary linsitinib

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
NFPA 704
0
2 0

Linsitinib price More Price(33)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 17708 Linsitinib ≥98% 867160-71-2 1mg $40 2024-03-01 Buy
Cayman Chemical 17708 Linsitinib ≥98% 867160-71-2 5mg $119 2024-03-01 Buy
Cayman Chemical 17708 Linsitinib ≥98% 867160-71-2 10mg $218 2024-03-01 Buy
Usbiological 015629 Linsitinib 867160-71-2 5mg $245 2021-12-16 Buy
TRC L469020 Linsitinib 867160-71-2 100mg $990 2021-12-16 Buy
Product number Packaging Price Buy
17708 1mg $40 Buy
17708 5mg $119 Buy
17708 10mg $218 Buy
015629 5mg $245 Buy
L469020 100mg $990 Buy

Linsitinib Chemical Properties,Uses,Production

Description

Linsitinib (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 vitro

OSI-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 vivo

OSI-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.

Description

The 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.

Uses

Linsitinib 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.

Definition

ChEBI: 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.

target

IGF-1R

storage

Store at -20°C

References

1) 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

Raw materials

Preparation Products

Linsitinib Suppliers

Global( 146)Suppliers
Supplier Tel Email Country ProdList Advantage
Capot Chemical Co.,Ltd. 		571-85586718 +8613336195806 sales@capotchem.com China 29797 60
Hangzhou FandaChem Co.,Ltd. 		008657128800458; +8615858145714 fandachem@gmail.com China 9348 55
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 32480 60
Biochempartner 		0086-13720134139 candy@biochempartner.com CHINA 967 58
Changzhou PBpharmaceutical R&D Co.,Ltd 		0519-83990708 info@pbpharm.com CHINA 498 58
CONIER CHEM AND PHARMA LIMITED 		+8618523575427 sales@conier.com China 49390 58
career henan chemical co 		+86-0371-86658258 15093356674; factory@coreychem.com China 29826 58
Dideu Industries Group Limited 		+86-29-89586680 +86-15129568250 1026@dideu.com China 29220 58
Zhejiang J&C Biological Technology Co.,Limited 		+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10523 58
InvivoChem 		+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6393 58
Supplier Advantage
Capot Chemical Co.,Ltd. 		60
Hangzhou FandaChem Co.,Ltd. 		55
ATK CHEMICAL COMPANY LIMITED 		60
Biochempartner 		58
Changzhou PBpharmaceutical R&D Co.,Ltd 		58
CONIER CHEM AND PHARMA LIMITED 		58
career henan chemical co 		58
Dideu Industries Group Limited 		58
Zhejiang J&C Biological Technology Co.,Limited 		58
InvivoChem 		58

Related articles

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  • 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

View Lastest Price from Linsitinib manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Linsitinib pictures 2022-10-14 Linsitinib
867160-71-2
 US $0.00-0.00 / KG 1KG 98% 1Ton Henan Aochuang Chemical Co.,Ltd.
Linsitinib pictures 2020-01-09 Linsitinib
867160-71-2
 US $6.68 / KG 1KG 97%-99% 1kg-1000kg Career Henan Chemical Co
  • Linsitinib pictures
  • Linsitinib
    867160-71-2
  • US $0.00-0.00 / KG
  • 98%
  • Henan Aochuang Chemical Co.,Ltd.
  • Linsitinib pictures
  • Linsitinib
    867160-71-2
  • US $6.68 / KG
  • 97%-99%
  • Career Henan Chemical Co

Linsitinib Spectrum

Linsitinib(867160-71-2)1HNMR

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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 Linsitinib(OSI906) (1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol cis-3-[8-Amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutanol Linsitinib(OSI906) 3-(8-Amino-1-(2-phenylquinolin-7-yl)-2,3-dihydro-imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobuta LINSITINIB;OSI 906; OSI906 CS-190 OSI 906;OSI906 3-[8-AMINO-1-(2-PHENYLQUINOLIN-7-YL)IMIDAZO[1,5-A]PYRAZIN-3-YL]-1-METHYLCYCLOBUTAN-1-OL (1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutan-1-ol Linsitinib USP/EP/BP OSI-906 Cis-3-(8-Amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutan-1-ol 867160-71-2 Tyrosine Kinase Inhibitors Inhibitors Amines Aromatics Heterocycles Intermediates & Fine Chemicals Pharmaceuticals