Onalespib

Bezeichnung:Onalespib

CAS-Nr912999-49-6

Englisch Name:Onalespib

CBNumberCB32566420

SummenformelC24H31N3O3

Molgewicht409.52

MOL-Datei912999-49-6.mol

Onalespib physikalisch-chemischer Eigenschaften

Siedepunkt	605.7±55.0 °C(Predicted)
Dichte	1.237
storage temp.	Store at -20°C
Löslichkeit	insoluble in H2O; ≥13.25 mg/mL in DMSO; ≥47.7 mg/mL in EtOH with ultrasonic
Aggregatzustand	solid
pka	8.50±0.48(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

Onalespib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Einzelnachweise
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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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