ARV-771 Struktur

ARV-771

Bezeichnung:ARV-771

CAS-Nr1949837-12-0

Englisch Name:ARV-771

CBNumberCB13167639

SummenformelC49H60ClN9O7S2

Molgewicht986.65

MOL-Datei1949837-12-0.mol

ARV-771 physikalisch-chemischer Eigenschaften

Dichte	1.39±0.1 g/cm3(Predicted)
storage temp.	Sealed in dry,Store in freezer, under -20°C
Löslichkeit	DMSO:65.92(Max Conc. mg/mL);68.22(Max Conc. mM) DMF:20.0(Max Conc. mg/mL);20.7(Max Conc. mM) DMF:PBS (pH 7.2) (1:6):0.14(Max Conc. mg/mL);0.14(Max Conc. mM) Ethanol:55.0(Max Conc. mg/mL);56.92(Max Conc. mM)
Aggregatzustand	A crystalline solid
pka	13.61±0.46(Predicted)
Farbe	White to light yellow
InChIKey	PQOGZKGXGLHDGS-BZTQNJCZNA-N

Gefahreninformationscode (GHS)

ARV-771 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
ARV-771 is a BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2), respectively.
Verwenden
ARV-771 is an effective BET degrader of the PROTAC class.
Biologische Funktion
ARV-771, a von Hippel–Landau (VHL) E3 ligase-based BET PROTAC, is highly active against cellular models of CRPC. ARV-771 in these cells results in rapid BET protein degradation with DC50 (the drug concentration that results in 50% protein degradation) values <1 nM. Interestingly, ARV–771–mediated BET degradation leads to decreased both FL-AR and AR-V7 at the transcript level. In contrast, treating CRPC cells with BET inhibitors leads to the suppression of AR-V7 but not of FL-AR levels. Moreover, ARV-771 causes significantly greater apoptotic cell death than a BET inhibitor. ARV-771 dramatically suppresses the proliferation of castration-resistant prostate cancer models via inducing Von Hippel Lindau (VHL) E3 ligase-mediated degradation of BRDs and inhibiting AR signaling. A subsequent study has demonstrated that ARV-771 can also suppress the proliferation of mantle cell lymphoma cells via increasing the levels of tumour suppressors, including CDKN1A/p21, HEXIM1, and NOXA[1].
Biologische Aktivität
ARV-771 is a potent pan-(bromodomain and extra-terminal) BET degrader, a novel BET-PROTAC (proteolysis-targeting chimera), for BRD2(1), BRD2(2), BRD3(1) The Kd values of , BRD3(2), BRD4(1) and BRD4(2) were 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM and 7.6 nM, respectively.

target

td>

Target	Value
BRD2-BD2 (Cell-free assay)	4.7 nM(Kd)
BRD3-BD2 (Cell-free assay)	7.6 nM(Kd)
BRD4-BD2 (Cell-free assay)	7.6 nM(Kd)
BRD3-BD1 (Cell-free assay)	8.3 nM(Kd)
BRD4-BD1 (Cell-free assay)	9.6 nM(Kd)

Lager
Store at -20°C
Einzelnachweise
[1] Yuanfei Deng. “ARV-771 Acts as an Inducer of Cell Cycle Arrest and Apoptosis to Suppress Hepatocellular Carcinoma Progression.” Frontiers in Pharmacology (2022).

ARV-771 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

1949837-12-0, ARV-771 Verwandte Suche:

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