Linsitinib

ChemicalBook > CAS DataBase List > Linsitinib

Description In vitro In vivo

Product Name: Linsitinib
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
Formula Weight: 421.49
MOL File: 867160-71-2.mol

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Linsitinib Property

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.

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Warning

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 17708
Product name: Linsitinib
Purity: ≥98%
Packaging: 1mg
Price: $40
Updated: 2024/03/01

Cayman Chemical

Product number: 17708
Product name: Linsitinib
Purity: ≥98%
Packaging: 5mg
Price: $119
Updated: 2024/03/01

Cayman Chemical

Product number: 17708
Product name: Linsitinib
Purity: ≥98%
Packaging: 10mg
Price: $218
Updated: 2024/03/01

Usbiological

Product number: 015629
Product name: Linsitinib
Packaging: 5mg
Price: $245
Updated: 2021/12/16

TRC

Product number: L469020
Product name: Linsitinib
Packaging: 100mg
Price: $990
Updated: 2021/12/16

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Linsitinib Chemical Properties,Usage,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

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View Lastest Price from Linsitinib manufacturers

Henan Aochuang Chemical Co.,Ltd.

Product: Linsitinib 867160-71-2
Price: US $0.00-0.00/KG
Min. Order: 1KG
Purity: 98%
Supply Ability: 1Ton
Release date: 2022-10-13

Career Henan Chemical Co

Product: Linsitinib 867160-71-2
Price: US $6.68/KG
Min. Order: 1KG
Purity: 97%-99%
Supply Ability: 1kg-1000kg
Release date: 2020-01-08

867160-71-2, LinsitinibRelated Search:

Geldanamycin LFM-A13 Vorinostat (+)-Camptothecin lifitegrast Linagliptin Y27632 (hydrochloride) MK-2206 2HCl Erlotinib hydrochloride SCH772984 BMS-754807 Olaparib

OSI-906

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;OSI 906; OSI906

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

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

Cis-3-(8-Amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutan-1-ol

867160-71-2

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