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Onalespib (AT13387)
| Product Name | Onalespib (AT13387) |
| Price: | Inquiry |
| Catalog No.: | CN00138 |
| CAS No.: | 912999-49-6 |
| Molecular Formula: | C24H31N3O3 |
| Molecular Weight: | 409.52 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | CN1CCN(CC1)Cc1ccc2c(c1)CN(C2)C(=O)c1cc(C(C)C)c(cc1O)O |
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| Description | Onalespib (AT13387) is a potent inhibitor of Hsp90, with a Kd of 0.71 nM. |
| Target | HSP90:0.71 nM (Kd) |
| In Vitro | Onalespib (Compound 35) is a potent inhibitor of Hsp90, with Kd of 0.71 nM. Onalespib shows potent antiproliferative activity in HCT116 cells, with an IC50 of 31 nM. Onalespib also strongly inhibits the proliferation of a panel of human tumor cell lines, showing IC50 of < 100 nM[1]. Onalespib exhibits cytotoxic activity against many of the PPTP cell lines, with median IC50 of 41 nM[2]. |
| In Vivo | Onalespib (60 mg/kg, ip 3 days on and 3 days off for four cycles) shows antitumor activity in nude BALB/c mice bearing early stage HCT116 human colon carcinoma xenografts[1]. Onalespib (40 or 60 mg/kg, i.p.) induces significant differences in EFS distribution compared to controls in 17% evaluable solid tumor xenografts, but in none of the ALL xenografts[2]. |
| Cell Assay | In vitro testing is performed using DIMSCAN. Cells are incubated in the presence of Onalespib for 96 hours at concentrations from 1 nM to 10 μM[2]. |
| Animal Admin | HCT116 cells are injected SC into the right hind flank of male nude BALB/c mice. Tumours are apparent 7 to 10 days later. Mice are arranged into matched groups of 12 according to tumour volume giving a group mean of approximately 100 mm[3] at initiation of dosing. Tumour volumes are measured every 2 days. Statistical significance between groups is assessed using nonparametric one-way ANOVA. Mice are given the lactate salt of Onalespib using a repeated cycle of dosing of once per day for three days, no dose for three days, once per day for three days etc., for four dosing cycles at 60 mg/kg/dose (as free base equivalents) dissolved in 17.5% hydroxypropyl-β-cyclodextrin via the IP route. Control mice receive dose vehicle only via the same route. Tolerability is assessed by recording body weight, clinical observations and survival[1]. |
| Density | 1.2±0.1 g/cm3 |
| Boiling Point | 605.7±55.0 °C at 760 mmHg |
| Flash Point | 320.1±31.5 °C |
| Exact Mass | 409.236542 |
| PSA | 67.25000 |
| LogP | 1.52 |
| Vapour Pressure | 0.0±1.8 mmHg at 25°C |
| Storage condition | -20℃ |