AT13387 (Synonyms: AT-13387,Onalespib) |
Catalog No.GC13414
One-Click Copy Product Info
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AT13387 is a small-molecule, non-ansamycin HSP90 (heat shock protein 90) inhibitor that acts by targeting the AKT and ERK signaling pathways.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 912999-49-6
Sample solution is provided at 25 µL, 10mM.
AT13387 is a small-molecule, non-ansamycin HSP90 (heat shock protein 90) inhibitor that acts by targeting the AKT and ERK signaling pathways[1]. AT13387 inhibits tumor cell growth and migration and exerts synergistic anti-cancer effects when combined with radiotherapy[2]. AT13387 is commonly used in the study of non-small cell lung cancer (NSCLC)[3].
AT13387 (0.1 - 2.5µM, 72h) inhibited cell proliferation in glioblastoma cell lines in a dose-dependent manner (IC50 ≤ 0.25μM). AT13387 (0.4µM, 24h) significantly inhibited the proliferation and angiogenic potential of glioma cells[4].
AT13387 (5, 10mg/kg/day; 3 days; i.p.) significantly reduced tumor growth and prolonged both median and overall survival in the radiosensitive HCT116 human adenocarcinoma xenograft mouse model[2].
References:
[1] Riess J W, Reckamp K L, Frankel P, et al. Erlotinib and onalespib lactate focused on EGFR exon 20 insertion non-small cell lung cancer (NSCLC): a California Cancer Consortium Phase I/II Trial (NCI 9878)[J]. Clinical lung cancer, 2021, 22(6): 541-548.
[2] Spiegelberg D, Abramenkovs A, Mortensen A C L, et al. The HSP90 inhibitor Onalespib exerts synergistic anti-cancer effects when combined with radiotherapy: an in vitro and in vivo approach[J]. Scientific Reports, 2020, 10(1): 5923.
[3] Mooradian M J, Cleary J M, Giobbie‐Hurder A, et al. Dose‐escalation trial of combination dabrafenib, trametinib, and AT13387 in patients with BRAF‐mutant solid tumors[J]. Cancer, 2023, 129(12): 1904-1918.
[4] Canella A, Welker A M, Yoo J Y, et al. Efficacy of onalespib, a long-acting second-generation HSP90 inhibitor, as a single agent and in combination with temozolomide against malignant gliomas[J]. Clinical Cancer Research, 2017, 23(20): 6215-6226.
| Cell experiment [1]: | |
Cell lines | LN229, U251HF and A172 Glioblastoma cell lines |
Preparation Method | LN229, U251HF and A172 cells were seeded into 96 well plates and exposed to vehicle control (DMSO) or increasing concentrations of AT13387 (0.1 - 2.5μM) for 72h. Cell viability was measured using the WST-1 assay as per manufacturer’s instructions. |
Reaction Conditions | 0.1 - 2.5µM, 72h |
Applications | AT13387 inhibited cell proliferation in a dose-dependent manner, with an IC50 ≤ 0.25μM. |
| Animal experiment [2]: | |
Animal models | Radiosensitive HCT116 human adenocarcinoma xenograft mouse model |
Preparation Method | Female nu/nu Balb/c mice were housed under standard laboratory conditions and fed ad libitum. Tumor xenografts were formed by subcutaneous inoculation of approximately 1×106 HCT116 cells suspended in 100μL serum free cell culture medium in the right posterior leg. After approximately 10 days tumors had established (> 80mm3) and the treatment schedule started. HCT116 xenografted mice were divided into the following treatment groups: (i) control (N = 10), (ii) radiotherapy (N = 10) 3 × 2 Gy, (iii) AT13387 (N = 10) 3 × 10mg/kg AT13387, (iiii) AT13387 and 3 × 10mg/kg combined with 3 × 2 Gy (N = 10), (iv) AT13387 3 × 5mg/kg (N = 10), (v) AT13387 3 × 5mg/kg combined with 3 × 2 Gy (N = 10). Mice were injected intraperitoneally with 100µL AT13387 or (controls and radiation groups) with 100µL 17.5% β-Cyclodextrin on day 1, 2, and 3. Radiotherapy was given 6h after the drug treatment, performed under anesthesia on day 1, 2, and 3. Tumor size was measured every day with a digital caliper and survival analysis was performed after reaching the study endpoint of 1000mm3 tumor size. |
Dosage form | 5, 10mg/kg/day; 3 days; i.p. |
Applications | AT13387 significantly reduced tumor growth and prolonged both median and overall survival in the HCT116 mouse model. |
References: | |
| Cas No. | 912999-49-6 | SDF | |
| Synonyms | AT-13387,Onalespib | ||
| Chemical Name | (2,4-dihydroxy-5-propan-2-ylphenyl)-[5-[(4-methylpiperazin-1-yl)methyl]-1,3-dihydroisoindol-2-yl]methanone | ||
| Canonical SMILES | CC(C)C1=C(C=C(C(=C1)C(=O)N2CC3=C(C2)C=C(C=C3)CN4CCN(CC4)C)O)O | ||
| Formula | C24H31N3O3 | M.Wt | 409.5 |
| Solubility | ≥ 13.25 mg/mL in DMSO, ≥ 47.7 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.442 mL | 12.21 mL | 24.42 mL |
| 5 mM | 488.4 μL | 2.442 mL | 4.884 mL |
| 10 mM | 244.2 μL | 1.221 mL | 2.442 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)