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Purity: ≥98%
Onalespib (formerly AT13387; AT-13387; AT 13387) is a novel, orally bioavailable, long-acting and isoindole-based small-molecule HSP90 (heat shock protein 90) inhibitor with potential antitumor activity. It inhibits HSP90 with an IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Onalespib is being studies in clinical trials for men with CRPC, in particular thos who have failed treatment with abiraterone acetate
| ln Vitro |
Compound 35, onalespib, has a Kd of 0.71 nM, making it a strong inhibitor of Hsp90. In HCT116 cells, onalespib has strong antiproliferative activity with an IC50 of 31 nM. Additionally, onalespib exhibits substantial inhibition of a panel of human tumor cell lines' growth, with an IC50 of less than 100 nM[1]. Against numerous PPTP cell lines, onalespib demonstrates cytotoxic action, with a median IC50 of 41 nM[2].
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| ln Vivo |
Onalespib (60 mg/kg, intraperitoneal; 3 days on, 3 days off) exhibits anticancer efficacy in BALB/c nude mice expressing human colon carcinoma xenografts in the early stage [1]. In 17% of evaluable solid tumor xenografts, onalespib (40 or 60 mg/kg, ip) causes substantial variations in the EFS distribution with respect to controls, but not in any of the ALL xenografts[2].
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| References |
[1]. Woodhead AJ, et al. Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design. J Med Chem. 2010 Aug 26;53
[2]. Kang MH, et al. Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012 Jul 15;59(1):185-8 |
| Molecular Formula |
C24H31N3O3
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| Molecular Weight |
409.52
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| CAS # |
912999-49-6
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| Related CAS # |
Onalespib lactate;1019889-35-0
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| SMILES |
O=C(C1=CC(C(C)C)=C(O)C=C1O)N2CC3=C(C=C(CN4CCN(C)CC4)C=C3)C2
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| Chemical Name |
(2,4-dihydroxy-5-isopropylphenyl)(5-((4-methylpiperazin-1-yl)methyl)isoindolin-2-yl)methanone
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| Synonyms |
Onalespib lactate; AT13387; AT-13387; AT 13387; Onalespib;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2% DMSO+30% PEG 300+ddH2O: 10 mg/mL Solubility in Formulation 5: 16.67 mg/mL (40.71 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4419 mL | 12.2094 mL | 24.4188 mL | |
| 5 mM | 0.4884 mL | 2.4419 mL | 4.8838 mL | |
| 10 mM | 0.2442 mL | 1.2209 mL | 2.4419 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02503709 | Active, not recruiting | Drug: Onalespib Other: Pharmacological Study |
Advanced Malignant Solid Neoplasm Metastatic Malignant Solid Neoplasm |
National Cancer Institute (NCI) | April 8, 2016 | Phase 1 |
| NCT02474173 | Terminated | Drug: Onalespib Drug: Paclitaxel |
Advanced Breast Carcinoma Metastatic Breast Carcinoma |
National Cancer Institute (NCI) | January 15, 2016 | Phase 1 |
| NCT02572453 | Terminated Has Results | Drug: Onalespib | Recurrent Anaplastic Large Cell Lymphoma |
National Cancer Institute (NCI) | April 4, 2016 | Phase 2 |
| NCT02535338 | Active, not recruiting Has Results | Drug: Onalespib Lactate Other: Pharmacological Study |
Recurrent Lung Non-Small Cell Carcinoma |
National Cancer Institute (NCI) | January 21, 2016 | Phase 1 Phase 2 |
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