Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
SKU | Size | Availability | Price | Qty |
---|---|---|---|---|
L126224-1mg | 1mg | In stock | $15.90 | |
L126224-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $64.90 | |
L126224-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $90.90 | |
L126224-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $201.90 | |
L126224-100mg | 100mg | Available within 4-8 weeks(?) 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
Synonyms | Linsitinib (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 & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | Linsitinib 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 Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of Insulin-like growth factor I receptor;Inhibitor of Insulin receptor;Inhibitor of Insulin receptor-related receptor |
Note | Refer 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. |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
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 |
PubChem CID | 11640390 |
---|---|
CAS Registry No. | 867160-71-2 |
ChEMBL Ligand | CHEMBL1091644 |
Wikipedia | Linsitinib |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
K2415028 | Certificate of Analysis | Nov 19, 2024 | L126224 |
K1819045 | Certificate of Analysis | Apr 07, 2024 | L126224 |
K1819044 | Certificate of Analysis | Apr 07, 2024 | L126224 |
B2216162 | Certificate of Analysis | Feb 21, 2022 | L126224 |
Solubility | DMSO 84 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
---|
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, 1 (6): (1153-71). [PMID:21425998] [10.1021/op500134e] |