OSI-906 (Linsitinib) , ≥99% , 867160-71-2

CAS NO.：867160-71-2

Empirical Formula: C26H23N5O

Molecular Weight: 421.49

MDL number: MFCD12912153

EINECS: 1533716-785-6

PRODUCT Properties

• Melting point: >175°C (dec.)
• Density: 1.39
• storage temp.: -20°C
• solubility: Soluble in DMSO (up to 30 mg/ml)
• form: solid
• pka: 14.84±0.40(Predicted)
• color: Yellow
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
• InChIKey: PKCDDUHJAFVJJB-VLZXCDOPSA-N
• SMILES: [C@]1(C)(O)C[C@H](C2N3C=CN=C(N)C3=C(C3C=C4C(=CC=3)C=CC(C3=CC=CC=C3)=N4)N=2)C1

Description and Uses

The binding of insulin-like growth factor 1 (IGF-1) to the IGF-1 receptor (IGF-1R) promotes cell growth while inhibiting apoptotic pathways. Overexpression of IGF-1R is found in certain solid tumors and hematologic neoplasias. However, insulin receptor (InsR) signaling can compensate for IGF-1R inhibition. Linsitinib is a dual inhibitor of IGF-1R and InsR kinases (IC₅₀s = 35 and 75 nM, respectively). It also inhibits InsR-related receptor (IC₅₀ = 75 nM) but is without effect (IC₅₀ > 10 μM) against a large panel of other kinases. Linsitinib inhibits proliferation of a variety of tumor cell lines in vitro and has antitumor efficacy in an IGF-1R-driven xenograft mouse model when administered orally. A rapid, non-invasive method to predict the pharmacodynamic response to linsitinib has been reported.

Linsitinib is a small-molecule dual insulin-like growth factor-1 receptor (IGF-IR) and insulin receptor (IR) kinase inhibitor. IGF-I receptor (IGF-IR) has been implicated in the promotion of tumorigenesis, metastasis and resistance to cancer therapies and thus Linsitinib may be a useful anticancer agent. Potent IGF-1R inhibitor.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning