ChemicalBook > Product Catalog >Biochemical Engineering >Inhibitors >Cytoskeletal Signaling >HSP e.g. HSP90 inhibitors >Onalespib

Onalespib

Onalespib Structure
CAS No.
912999-49-6
Chemical Name:
Onalespib
Synonyms
CS-1866;AT-13387;Onalespib;ATI-13387;ATI13387X;AT13387, >=98%;Onalespib Lactate;AT13387(Onalespib);Onalespib (AT13387);ONALESPIB;ATI-13387
CBNumber:
CB32566420
Molecular Formula:
C24H31N3O3
Molecular Weight:
409.52
MOL File:
912999-49-6.mol
MSDS File:
SDS
Modify Date:
2024/7/2 8:55:06

Onalespib Properties

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)
color White to off-white

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319
Precautionary statements  P261-P305+P351+P338

Onalespib Chemical Properties,Uses,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.

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

Onalespib Preparation Products And Raw materials

Raw materials

Preparation Products

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(2,4-dihydroxy-5-isopropylphenyl)(5-((4-Methylpiperazin-1-yl)Methyl)isoindolin-2-yl)Methanone AT-13387 4-({5-[(4-Methylpiperazin-1-yl)Methyl]-2,3-dihydro-1H-isoindol-2-yl}carbonyl)-6-(propan-2-yl)benzene-1,3-diol [1,3-Dihydro-5-[(4-methyl-1-piperazinyl)methyl]-2H-isoindol-2-yl][2,4-dihydroxy-5-(1-methylethyl)phenyl]methanone Onalespib Onalespib (AT13387) [1,3-Dihydro-5-[(4-methyl-1-piperazinyl)methyl]-2H-isoindol-2-yl][2,4-dihydroxy-5-(1-methylethyl)phenyl]methanone AT13387 AT13387, >=98% Onalespib Lactate (2,4-dihydroxy-5-isopropylphenyl)(5-((4-Methylpiperazin-1-yl)Methyl)isoindolin-2-yl)Methanone USP/EP/BP Methanone, [1,3-dihydro-5-[(4-methyl-1-piperazinyl)methyl]-2H-isoindol-2-yl][2,4-dihydroxy-5-(1-methylethyl)phenyl]- ONALESPIB;ATI-13387 ATI-13387 (2,4-dihydroxy-5-propan-2-ylphenyl)-[5-[(4-methylpiperazin-1-yl)methyl]-1,3-dihydroisoindol-2-yl]methanone AT13387(Onalespib) CS-1866 ATI13387X Onalespib AT-13387 AT13387 912999-49-6 12999-49-6 Inhibitor Inhibitors