GLPBio

AT13387

Catalog No.: GC13414Purity:>99.50%Synonyms: AT-13387,Onalespib
COASDSData SheetNMR
AT13387 is a small-molecule, non-ansamycin HSP90 (heat shock protein 90) inhibitor that acts by targeting the AKT and ERK signaling pathways.

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AT13387
Cas No.: 912999-49-6
10mM (in 1mL DMSO)In Stock
$84.00
1
5mgIn Stock
$74.00
1
10mgIn Stock
$108.00
1
50mgIn Stock
$249.00
1
100mgIn Stock
$455.00
1
500mgIn Stock
$1,260.00
1
1gIn Stock
$2,058.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citations

1 publicationsPublications from researchers using this product

Description

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.

Protocol

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:
[1] 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.
[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.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData SheetNMR

Chemical Properties

CAS No.
912999-49-6
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
SMILES
CC(C)C1=C(C=C(C(=C1)C(=O)N2CC3=C(C2)C=C(C=C3)CN4CCN(CC4)C)O)O
Molecular Formula
C24H31N3O3
Molecular Weight
409.5
Solubility
≥ 13.25 mg/mL in DMSO, ≥ 47.7 mg/mL in EtOH with ultrasonic
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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