OSI-906 (Linsitinib) - ≥99%, high purity , CAS No.867160-71-2, Inhibitor of Insulin-like growth factor I receptor;Inhibitor of Insulin receptor;Inhibitor of Insulin receptor-related receptor

Item Number
L126224
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SKUSizeAvailabilityPrice Qty
L126224-1mg
1mg
In stock
$15.90
L126224-5mg
5mg
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Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$64.90
L126224-10mg
10mg
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$90.90
L126224-50mg
50mg
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Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$201.90
L126224-100mg
100mg
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Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$280.90

Potent and selective dual IGF-1R and Insulin Receptor kinase inhibitor

Basic Description

SynonymsLinsitinib (USAN/INN) | Cis-3-(8-Amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutan-1-ol | HMS3295G15 | Kinome_3532 | CHEBI:91402 | (1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol | S
Specifications & PurityMoligand™, ≥99%
Biochemical and Physiological MechanismsLinsitinib is highly potent, orally efficacious and highly selective, dual ATP-competitive tyrosine kinase inhibitor of insulin-like growth factor-1 receptor (IGF-1R) (IC50: 35 nM) and insulin receptor (IR) (IC50: 75 nM).Potent and selective dual IGF-1R (
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of Insulin-like growth factor I receptor;Inhibitor of Insulin receptor;Inhibitor of Insulin receptor-related receptor
NoteRefer to SDS for further information Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Linsitinib is a potent, selective insulin-like growth factor-1 receptor (IGF-1R, IC50 = 35 nM) and insulin receptor (IR, IC50 = 75 nM) kinase inhibitor which works to block the autophosphorylation of IGF-1R and IR. Additionally, in vitro studies of Linsitinib have demonstrated its ability to inhibit the proliferation of multiple tumor cell lines.
Linsitinib 是一种选择性的 IGF-1R 抑制剂,IC50 值为 35 nM,也适度地作用于 InsR,IC50 值为 75 nM;对 Abl,ALK,BTK,EGFR,FGFR1/2,PKA 等没有作用。

Associated Targets(Human)

IGF1R Tclin Insulin-like growth factor 1 receptor (10 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
INSRR Tchem Insulin receptor-related protein (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
INSR Tclin Insulin receptor (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 3-[8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutan-1-ol
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)
InChi Key PKCDDUHJAFVJJB-UHFFFAOYSA-N
Canonical SMILES CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O
Isomeric SMILES CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O
PubChem CID 11640390
Molecular Weight 421.51

Certificates

Certificate of Analysis(COA)

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4 results found

Lot NumberCertificate TypeDateItem
K2415028Certificate of AnalysisNov 19, 2024 L126224
K1819045Certificate of AnalysisApr 07, 2024 L126224
K1819044Certificate of AnalysisApr 07, 2024 L126224
B2216162Certificate of AnalysisFeb 21, 2022 L126224

Chemical and Physical Properties

SolubilityDMSO 84 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

Related Documents

References

1. Mulvihill MJ, Cooke A, Rosenfeld-Franklin M, Buck E, Foreman K, Landfair D, O'Connor M, Pirritt C, Sun Y, Yao Y et al..  (2009)  Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor..  Future Med Chem,  (6): (1153-71).  [PMID:21425998] [10.1021/op500134e]

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