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AB273391

Linsitinib (OSI-906)

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MW 421.5 Da, Purity 98%. Potent and selective dual IGF-1R (IC50 = 35 nM in cell-free assay) and Insulin Receptor (IC50 = 75 nM in cell-free assay) kinase inhibitor. Inactive towards Abl, ALK, BTK, EGFR, FGFR1/2 and PKA. Displayed <50% inhibition at 1 μM against a panel of 88 kinases. Blocks IGF-1R autophosphorylation and downstream activation of Akt, ERK1/2 and S6 kinase. Blocks tumor cell line proliferation. Blocks IGF-1R driven tumor xenograft growth.

View Alternative Names

EC 2.7.11.1, Germinal center kinase like kinase, Germinal center kinase-related protein kinase, KHS, Kinase homologous to SPS1/STE20, MAP4K3, MAPK/ERK kinase kinase kinase 3, MAPK/ERK kinase kinase kinase 5, MAPKKKK3, MEK kinase kinase 3, MEK kinase kinase 5, MEKKK 3, MEKKK 5, RAB8IPL1, mitogen-activated protein kinase kinase kinase kinase 3

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Chemical Structure - Linsitinib (OSI-906) (AB273391)
  • Chemical Structure

Lab

Chemical Structure - Linsitinib (OSI-906) (AB273391)

Chemical structure of Linsitinib (OSI-906), 867160-71-2

Key facts

CAS number

867160-71-2

Purity

98%

Form

Solid

form

Molecular weight

421.5 Da

Molecular formula

C<sub>2</sub><sub>6</sub>H<sub>2</sub><sub>3</sub>N<sub>5</sub>O

PubChem

11640390

Nature

Synthetic

Solubility

Soluble in DMSO to 50 mM

Biochemical name

Linsitinib

Biological description

Potent and selective dual IGF-1R (IC50 = 35 nM in cell-free assay) and Insulin Receptor (IC50 = 75 nM in cell-free assay) kinase inhibitor. Inactive towards Abl, ALK, BTK, EGFR, FGFR1/2 and PKA. Displayed <50% inhibition at 1 μM against a panel of 88 kinases. Blocks IGF-1R autophosphorylation and downstream activation of Akt, ERK1/2 and S6 kinase. Blocks tumor cell line proliferation. Blocks IGF-1R driven tumor xenograft growth.

Canonical 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(23)25)18-8-7-17-9-10-20(29-21(17)13-18)16-5-3-2-4-6-16/h2-13,19,32H,14-15H2,1H3,(H2,27,28)

InChiKey

PKCDDUHJAFVJJB-UHFFFAOYSA-N

IUPAC Name

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

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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions
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Product protocols

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