Onalespib
- Product Name
- Onalespib
- CAS No.
- 912999-49-6
- Chemical Name
- Onalespib
- Synonyms
- CS-1866;AT-13387;ATI13387X;Onalespib;ATI-13387;AT13387, >=98%;Onalespib Lactate;AT13387(Onalespib);Onalespib (AT13387);ONALESPIB;ATI-13387
- CBNumber
- CB32566420
- Molecular Formula
- C24H31N3O3
- Formula Weight
- 409.52
- MOL File
- 912999-49-6.mol
Onalespib Property
- Boiling point:
- 605.7±55.0 °C(Predicted)
- Density
- 1.237
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; ≥13.25 mg/mL in DMSO; ≥47.7 mg/mL in EtOH with ultrasonic
- form
- solid
- pka
- 8.50±0.48(Predicted)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 10655
- Product name
- Onalespib
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 10655
- Product name
- Onalespib
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $151
- Updated
- 2024/03/01
- Product number
- 10655
- Product name
- Onalespib
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $278
- Updated
- 2024/03/01
- Product number
- 10655
- Product name
- Onalespib
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $586
- Updated
- 2024/03/01
- Product number
- FA145338
- Product name
- AT-13387
- Packaging
- 25mg
- Price
- $595
- Updated
- 2021/12/16
Onalespib Chemical Properties,Usage,Production
Description
Onalespib, also known as AT13387, is a selective inhibitor of Hsp90 (IC50 = 18 nM). It induces the degradation of specific Hsp90 client proteins, including mutant EGFR, for up to seven days in tumor cell lines in vitro and up to three days in vivo. Onalespib is retained in tumor xenografts and is efficacious in a range of xenograft models. It differs from other HSP90 inhibitors in its longer duration of target inhibition and its favorable toxicity profile in phase I studies in patients with refractory solid tumors.
Definition
ChEBI: Onalespib is a member of the class of isoindoles that is isoindole in which the amino group has been acylated by a 2,4-dihydroxy-5-isopropylbenzoyl group and in which position 5 of the isoidole moiety has been substituted by a (4-methylpiperazin-1-yl)methyl group. A second-generation Hsp90 inhibitor. It has a role as a Hsp90 inhibitor and an antineoplastic agent. It is a member of resorcinols, a member of benzamides, a tertiary carboxamide, a member of isoindoles and a N-alkylpiperazine.
target
Hsp90
Mode of action
Onalespib selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins and has been used as a biomarker of HSP90 inhibition.
References
Efficacy of Onalespib, a Long-Acting Second-Generation HSP90 Inhibitor, as a Single Agent and in Combination with Temozolomide against Malignant Gliomas
https://pubchem.ncbi.nlm.nih.gov/compound/Onalespib