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.
867160-71-2
98%
Solid
421.5 Da
C26H23N5O
11640390
Synthetic
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
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.
867160-71-2
98%
Solid
421.5 Da
C26H23N5O
11640390
Synthetic
Soluble in DMSO to 50 mM.
Linsitinib
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.
CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O
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)
PKCDDUHJAFVJJB-UHFFFAOYSA-N
3-[8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutan-1-ol
Ambient - Can Ship with Ice
-20°C
-20°C
Store under desiccating conditions
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Chemical structure of Linsitinib (OSI-906), 867160-71-2
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