OSI-906

Catalog No. A11053

OSI-906是一种选择性IGF-1R抑制剂，在无细胞试验中IC50为35 nM；对InsR抑制作用适中，IC50为75 nM，对Abl，ALK，BTK，EGFR， FGFR1/2，PKA等没有抑制活性。

Product Citations

Masao Kakoki, .et al. Cyanocobalamin prevents cardiomyopathy in type 1 diabetes by modulating oxidative stress and DNMT-SOCS1/3-IGF-1 signaling, Communications Biology, 2021, 4:775
Nakamura T, .et al. Naturally Occurring Hair Growth Peptide: Water-Soluble Chicken Egg Yolk Peptides Stimulate Hair Growth Through Induction of Vascular Endothelial Growth Factor Production, J Med Food, 2018, Jul;21(7):701-708 PMID: 29583066
Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
Takata N, .et al. IGF-2/IGF-1R signaling has distinct effects on Sox1, Irx3, and Six3 expressions during ES cell derived-neuroectoderm development in vitro, In Vitro Cell Dev Biol Anim., 2016, May;52(5):607-15 PMID: 26956358

Technical details

Catalog Num	A11053
M. Wt	421.5
Formula	C26H23N5O
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	867160-71-2
Synonyms	OSI906, linsitinib
SMILES	CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O

Biological Activity

OSI-906是一种选择性IGF-1R抑制剂，在无细胞试验中IC50为35 nM；对InsR抑制作用适中，IC50为75 nM，对Abl，ALK，BTK，EGFR， FGFR1/2，PKA等没有抑制活性。

Targets

Target	Value
IGF-1R	IC50: 35nM
Insulin Receptor	IC50: 75nM
IRR	IC50: 75nM
Abl	IC50: >10μM
ALK	IC50: >10μM
BTK	IC50: >10μM
EGFR	IC50: >10μM
EphA1	IC50: >10μM
EphB1	IC50: >10μM
FES	IC50: >10μM
FGFR1	IC50: >10μM
FGFR2	IC50: >10μM
Fyn	IC50: >10μM
PKA	IC50: >10μM
PKCα	IC50: >10μM
ROCK1	IC50: >10μM
IRAK4	IC50: >10μM
JAK2	IC50: >10μM
KDR	IC50: >10μM
LCK	IC50: >10μM
LynA	IC50: >10μM
LynB	IC50: >10μM
Met	IC50: >10μM
TrkA	IC50: >10μM
PDGFRα	IC50: >10μM
PDGFRβ	IC50: >10μM
FAK	IC50: >10μM
BRK	IC50: >10μM
RET	IC50: >10μM
Pim1	IC50: >10μM
CDK1	IC50: >10μM
DYRK2	IC50: >10μM
Src	IC50: >10μM
Tek	IC50: >10μM
MEK1	IC50: >10μM
Akt1	IC50: >10μM
Akt2	IC50: >10μM
AuroraA	IC50: >10μM
AuroraB	IC50: >10μM
PDK-1	IC50: >10μM
PLK1	IC50: >10μM
p38α	IC50: >10μM
ERK1	IC50: >10μM
GSK-3α	IC50: >10μM
p70S6K	IC50: >10μM

Solubility *

In vitro (25°C)	DMSO	80 mg/mL (189.8 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	5%DMSO+40%PEG300+5%Tween80+50%ddH2O	5.93 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	23.72 mL	118.62 mL	237.25 mL
0.5 mM	4.74 mL	23.72 mL	47.45 mL
1 mM	2.37 mL	11.86 mL	23.72 mL
5 mM	0.47 mL	2.37 mL	4.74 mL

*The above data is based on the productmolecular weight 421.5 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.