Molecular structure of Linsitinib, CAS Number: 867160-71-2
Linsitinib (CAS 867160-71-2)
See product citations (1)
Alternate Names:
OSI-906
Application:
Linsitinib is a selective inhibitor of IGF-IR and IR kinase
CAS Number:
867160-71-2
Molecular Weight:
421.49
Molecular Formula:
C26H23N5O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Linsitinib is a potent, selective IGF-1R (insulin-like growth factor-1 receptor, IC50 = 35 nM) and insulin receptor (IR, IC50 = 75 nM) kinase inhibitor which works to block the autophosphorylation of IGF-1R and IR. Linsitinib competitively inhibits the ATP-binding site of the IGF-1R and IR tyrosine kinases. This inhibition blocks the phosphorylation and activation of the receptors, thereby disrupting downstream signaling pathways that are vital for cell division and growth, angiogenesis, and survival mechanisms in cells. Additionally, in vitro studies of Linsitinib have demonstrated its ability to inhibit the proliferation of multiple tumor cell lines. Tyrosine kinase inhibitors function by blocking the enzyme activity for initiating the signaling pathways that promote cell growth and survival. By inhibiting these receptors, linsitinib interferes with the growth of cancer cells.
Linsitinib (CAS 867160-71-2) References
- Linsitinib (OSI-906) antagonizes ATP-binding cassette subfamily G member 2 and subfamily C member 10-mediated drug resistance. | Zhang, H., et al. 2014. Int J Biochem Cell Biol. 51: 111-9. PMID: 24726739
- Mechanism of repression of 11β-hydroxysteroid dehydrogenase type 1 by growth hormone in 3T3-L1 adipocytes. | Muraoka, T., et al. 2014. Endocr J. 61: 675-82. PMID: 24759003
- Effectiveness of inhibitor rapamycin, saracatinib, linsitinib and JNJ-38877605 against human prostate cancer cells. | Li, W., et al. 2015. Int J Clin Exp Med. 8: 6563-7. PMID: 26131286
- Mass balance, pharmacokinetics, and metabolism of linsitinib in cancer patients. | Poondru, S., et al. 2016. Cancer Chemother Pharmacol. 77: 829-37. PMID: 26972330
- A Randomized Phase II Study of Linsitinib (OSI-906) Versus Topotecan in Patients With Relapsed Small-Cell Lung Cancer. | Chiappori, AA., et al. 2016. Oncologist. 21: 1163-1164. PMID: 27694157
- Overcoming Linsitinib intrinsic resistance through inhibition of nuclear factor-κB signaling in esophageal squamous cell carcinoma. | Wu, J., et al. 2017. Cancer Med. 6: 1353-1361. PMID: 28440057
- A phase 2 study of OSI-906 (linsitinib, an insulin-like growth factor receptor-1 inhibitor) in patients with asymptomatic or mildly symptomatic (non-opioid requiring) metastatic castrate resistant prostate cancer (CRPC). | Barata, P., et al. 2018. Invest New Drugs. 36: 451-457. PMID: 29476383
- A Phase I Dose-Escalation Study of Linsitinib (OSI-906), a Small-Molecule Dual Insulin-Like Growth Factor-1 Receptor/Insulin Receptor Kinase Inhibitor, in Combination with Irinotecan in Patients with Advanced Cancer. | Davis, SL., et al. 2018. Oncologist. 23: 1409-e140. PMID: 30139840
- IGF-1R pathway activation as putative biomarker for linsitinib therapy to revert tamoxifen resistance in ER-positive breast cancer. | Kruger, DT., et al. 2020. Int J Cancer. 146: 2348-2359. PMID: 31490549
- The RNA m6A Reader YTHDF2 Maintains Oncogene Expression and Is a Targetable Dependency in Glioblastoma Stem Cells. | Dixit, D., et al. 2021. Cancer Discov. 11: 480-499. PMID: 33023892
- A phase-1 trial of linsitinib (OSI-906) in combination with bortezomib and dexamethasone for the treatment of relapsed/refractory multiple myeloma. | Khan, S., et al. 2021. Leuk Lymphoma. 62: 1721-1729. PMID: 33509009
- IGF1-mediated HOXA13 overexpression promotes colorectal cancer metastasis through upregulating ACLY and IGF1R. | Qiao, C., et al. 2021. Cell Death Dis. 12: 564. PMID: 34075028
- Therapeutic IGF-I receptor inhibition alters fibrocyte immune phenotype in thyroid-associated ophthalmopathy. | Fernando, R., et al. 2021. Proc Natl Acad Sci U S A. 118: PMID: 34949642
- Dual IGF1R/IR inhibitors in combination with GD2-CAR T-cells display a potent anti-tumor activity in diffuse midline glioma H3K27M-mutant. | de Billy, E., et al. 2022. Neuro Oncol. 24: 1150-1163. PMID: 34964902
- Human Kinase IGF1R/IR Inhibitor Linsitinib Controls the In Vitro and Intracellular Growth of Mycobacterium tuberculosis. | Wang, H., et al. 2022. ACS Infect Dis. 8: 2019-2027. PMID: 36048501
Inhibitor of:
A2LD1, BRSK2, BZW1, DDR2, IGF-I, IGF-IA, IGF-IB, IGF-II, IGF-IIR, IGF-IR, IGF-IRα, IGF-IRβ, IGF2AS, IGFBP3, IGFBP4, IGFBP6, IGFBPL1, IGFL2, IGRP, Insulin II, insulin R, IRS-1, Ras GAP, RIA1, RREB1, Shc4, and Speedy B.Activator of:
PAPP-A.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Linsitinib, 5 mg | sc-396762 | 5 mg | $143.00 | |||
Linsitinib, 10 mg | sc-396762A | 10 mg | $260.00 |