AT13387 (CAS 912999-49-6)
QUICK LINKS
AT13387 is a selective potent heat shock protein 90 (Hsp90) inhibitor with IC50 of 18 nM in A375 cells. The Kd for AT13387 binding is 0.7 nM. This compares to a Kd of 6.7 nM for the binding of the ansamycin 17-AAG to the same site. The mean stoichio metry of binding for AT13387 is 1.03. The inhibition of a number of isolated kinases by AT13387 is also investigated including CDK 1, CDK 2, CDK4, FGFR3, PKB-b, JAK2, VEGFR2, PDGFR-b and Aurora B. None of the tested kinases are significantly inhibited at concentrations below 30 μM. AT13387 is a potent inhibitor of the proliferat ion and survival of many different cell lines (such as MES-SA cell line) from a variety of different tumor types. Across a panel of 30 tumor cell lines, AT13387 potently inhibits cell proliferation (GI50 of 13-260 nM). AT13387 inhibits proliferation of the non-tumorigenic human prostate epithelial cell line PNT2 (GI50 value of 480 nM).
AT13387 (CAS 912999-49-6) References
- Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program. | Kang, MH., et al. 2012. Pediatr Blood Cancer. 59: 185-8. PMID: 21538821
- The heat shock protein 90 inhibitor, AT13387, displays a long duration of action in vitro and in vivo in non-small cell lung cancer. | Graham, B., et al. 2012. Cancer Sci. 103: 522-7. PMID: 22181674
- The HSP90 inhibitor, AT13387, is effective against imatinib-sensitive and -resistant gastrointestinal stromal tumor models. | Smyth, T., et al. 2012. Mol Cancer Ther. 11: 1799-808. PMID: 22714264
- A novel Hsp90 inhibitor AT13387 induces senescence in EBV-positive nasopharyngeal carcinoma cells and suppresses tumor formation. | Chan, KC., et al. 2013. Mol Cancer. 12: 128. PMID: 24156782
- Inhibition of HSP90 by AT13387 delays the emergence of resistance to BRAF inhibitors and overcomes resistance to dual BRAF and MEK inhibition in melanoma models. | Smyth, T., et al. 2014. Mol Cancer Ther. 13: 2793-2804. PMID: 25349308
- The novel HSP90 inhibitor AT13387 potentiates radiation effects in squamous cell carcinoma and adenocarcinoma cells. | Spiegelberg, D., et al. 2015. Oncotarget. 6: 35652-66. PMID: 26452257
- The succinct synthesis of AT13387, a clinically relevant Hsp90 inhibitor. | Kaur, J., et al. 2019. Synth Commun. 49: 1436-1443. PMID: 33093687
- The Heat Shock Protein 90 Inhibitor, AT13387, Protects the Alveolo-Capillary Barrier and Prevents HCl-Induced Chronic Lung Injury and Pulmonary Fibrosis. | Colunga Biancatelli, RML., et al. 2022. Cells. 11: PMID: 35326496
- Dose-escalation trial of combination dabrafenib, trametinib, and AT13387 in patients with BRAF-mutant solid tumors. | Mooradian, MJ., et al. 2023. Cancer. 129: 1904-1918. PMID: 37042037
- Phase Ib study of HSP90 inhibitor, onalespib (AT13387), in combination with paclitaxel in patients with advanced triple-negative breast cancer. | Williams, NO., et al. 2023. Ther Adv Med Oncol. 15: 17588359231217976. PMID: 38152697
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
AT13387, 10 mg | sc-364415 | 10 mg | $555.00 | |||
AT13387, 50 mg | sc-364415A | 50 mg | $1606.00 |