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OSI 906AA

Linsitinib

CAS: 867160-71-2

Molecular Formula: C26H23N5O

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OSI 906AA - Names and Identifiers

Name Linsitinib
Synonyms OSI-906
OSI 906AA
Linsitinib
OSI-906 Linsitinib
cis-3-[8-Amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutanol
Cyclobutanol, 3-[8-aMino-1-(2-phenyl-7-quinolinyl)iMidazo[1,5-a]pyrazin-3-yl]-1-Methyl-, cis-
(1s,3r)-3-[4-aMino-3-(2-phenylquinolin-7-yl)iMidazo[1,5-a]pyrazin-1-yl]-1-Methylcyclobutan-1-ol
(1S,3r)-3-((S)-8-aMino-1-(2-phenylquinolin-7-yl)-2,3-dihydroiMidazo[1,5-a]pyrazin-3-yl)-1-Methylcyclobutanol
CAS 867160-71-2
EINECS 1533716-785-6

OSI 906AA - Physico-chemical Properties

Molecular FormulaC26H23N5O
Molar Mass421.49
Density1.39
Melting Point>175°C (dec.)
Solubility Soluble in DMSO (up to 30 mg/ml)
Appearancesolid
ColorYellow
pKa14.84±0.40(Predicted)
Storage Condition-20°C
StabilityStable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
In vitro studyOSI-906 inhibited IGF-IR activation of autophosphorylation and downstream signaling proteins AKT, ERK1/2 and S6 kinase with an IC50 of 0.028 to 0.13 μm. OSI-906 the target protein forms an intermediate structural morphology by interacting with the C- helix. OSI-906 effect on liver microsomes, with good metabolic stability. OSI-906 concentration of 1 m, complete inhibition of IR and IGF-IR phosphorylation. OSI-906 inhibits proliferation of several tumor cell lines, including non-small cell lung cancer and colorectal cancer (CRC) tumor cell lines, with EC50 of 0.021 to 0.810 μm.
OSI-906 inhibited IGF-IR activation of autophosphorylation and downstream signaling proteins AKT, ERK1/2 and S6 kinases with an IC50 of 0.028 to 0.13 μm. OSI-906 the target protein forms an intermediate structural morphology by interacting with the C- helix. OSI-906 effect on liver microsomes, with good metabolic stability. OSI-906 concentration of 1 m, complete inhibition of IR and IGF-IR phosphorylation. OSI-906 inhibits proliferation of several tumor cell lines, including non-small cell lung cancer and colorectal cancer (CRC) tumor cell lines, with EC50 of 0.021 to 0.810 μm.
In vivo studyOSI-906 on IGF-IR-driven xenograft tumor mouse model, inhibit tumor growth, at a dose of 75 mg/kg treatment, resulting in 100% TGI and 55% decline, at a dose of 25 mg/kg treatment, results in 60% TGI, no regression. Treatment of dogs, rats and mice OSI-906 induced different elimination half-lives of 1.18 hours, 2.64 hours and 2.14 hours, respectively. OSI-906 female Sprague-Dawley rats and female CD-1 mice were treated individually at different doses, once a day, and the Vmax values were not proportional to the OSI-906 dose. OSI-906 according to the dose of 25 mg/kg treatment for 12 days, improve the blood sugar value. OSI-906 treatment of a IGF-IR-driven human full-length human IGF-IR (LISN) transplanted mouse model alone at a dose of 75 mg/kg maximally inhibited phosphorylation by IGF-IR (80%) between 4 and 24 hours, plasma drug concentrations ranged from 26.6 to 4.77 μm. OSI-906 at a dose of 60 mg/kg alone in NCI-H292 transplanted mice, 2,4,24 hours, inhibition of sugar absorption. OSI-906 in NCI-H292 transplantation mouse model, inhibit tumor growth.
OSI-906 Inhibition of tumor growth in a IGF-IR-driven xenograft mouse model, treated at a dose of 75 mg/kg, resulting in 100% TGI and 55% regression, treated at a dose of 25 mg/kg, resulting in 60% TGI, there was no recession. Treatment of dogs, rats and mice OSI-906 induced different elimination half-lives of 1.18 hours, 2.64 hours and 2.14 hours, respectively. OSI-906 female Sprague-Dawley rats and female CD-1 mice were treated individually at different doses, once a day, and the V max value was not proportional to the OSI-906 dose. OSI-906 according to the dose of 25 mg/kg treatment for 12 days, improve the blood sugar value. OSI-906 treatment of a IGF-IR-driven human full-length human IGF-IR (LISN) transplanted mouse model alone at a dose of 75 mg/kg maximally inhibited phosphorylation by IGF-IR (80%) between 4 and 24 hours, plasma drug concentrations ranged from 26.6 to 4.77 μm. OSI-906 at a dose of 60 mg/kg alone in NCI-H292 transplanted mice, 2,4,24 hours, inhibition of sugar absorption. OSI-906 in NCI-H292 transplantation mouse model, inhibit tumor growth.

OSI 906AA - Preparation solution concentration reference

 1mg5mg10mg
1 mM2.372 ml11.862 ml23.724 ml
5 mM0.474 ml2.372 ml4.745 ml
10 mM0.237 ml1.186 ml2.372 ml
5 mM0.047 ml0.237 ml0.474 ml
Last Update:2024-01-02 23:10:35
OSI 906AA
Supplier List
Shanghai Macklin Biochemical Co., Ltd
Featured ProductsSpot supply
Product Name: OSI-906 Visit Supplier Webpage Request for quotation
CAS: 867160-71-2
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
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Shanghai Amole Biotechnology Co., Ltd.
Multiple SpecificationsSpot supply
Product Name: Linsitinib Request for quotation
CAS: 867160-71-2
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
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SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
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CAS: 867160-71-2
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
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MedChemExpress (MCE)
Multiple SpecificationsSpot supply
Product Name: OSI-906 Visit Supplier Webpage Request for quotation
CAS: 867160-71-2
Tel: 609-228-6898
Email: sales@medchemexpress.com
     tech@medchemexpress.com
Mobile: 609-228-6898
SKYRUN INDUSTRIAL CO.,LTD
Spot supply
Product Name: Linsitinib Visit Supplier Webpage Request for quotation
CAS: 867160-71-2
Tel: +86 0571-86722205
Email: sales@chinaskyrun.com
Mobile: +8618958170122
QQ: 2531159185 Click to send a QQ messageSend QQ message
Wechat: chinaskyrun
Shanghai Yuanye Bio-Technology Co., Ltd.
Product Name: OSI-906 (Linsitinib) Visit Supplier Webpage Request for quotation
CAS: 867160-71-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
Shanghai Macklin Biochemical Co., Ltd
Featured ProductsSpot supply
Product Name: OSI-906 Visit Supplier Webpage Request for quotation
CAS: 867160-71-2
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
Shanghai Amole Biotechnology Co., Ltd.
Multiple SpecificationsSpot supply
Product Name: Linsitinib Request for quotation
CAS: 867160-71-2
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365 Click to send a QQ message
Wechat: 18916960931
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
Product Name: OSI-906 (Linsitinib) Visit Supplier Webpage Request for quotation
CAS: 867160-71-2
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
WhatsApp: +86-18621343501
MedChemExpress (MCE)
Multiple SpecificationsSpot supply
Product Name: OSI-906 Visit Supplier Webpage Request for quotation
CAS: 867160-71-2
Tel: 609-228-6898
Email: sales@medchemexpress.com
     tech@medchemexpress.com
Mobile: 609-228-6898
SKYRUN INDUSTRIAL CO.,LTD
Spot supply
Product Name: Linsitinib Visit Supplier Webpage Request for quotation
CAS: 867160-71-2
Tel: +86 0571-86722205
Email: sales@chinaskyrun.com
Mobile: +8618958170122
QQ: 2531159185 Click to send a QQ messageSend QQ message
Wechat: chinaskyrun
Shanghai Yuanye Bio-Technology Co., Ltd.
Product Name: OSI-906 (Linsitinib) Visit Supplier Webpage Request for quotation
CAS: 867160-71-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
View History
OSI 906AA
Metozolv ODT
分散黄114
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