[CAS NO. 1818885-28-7]  ARV-825

Ships within Stock Price Qty Total
$0.00
$0.00
Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis
request a quote
If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1818885-28-7]

Store
Catalog
SLK-S8297
Brand
Selleck
CAS
1818885-28-7

DESCRIPTION [1818885-28-7]

Overview

MDLMFCD29472237
Molecular Weight923.43
Molecular FormulaC46H47ClN8O9S
SMILESCC1=NN=C2N1C(SC(C)=C3C)=C3C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(NC5=CC=C(OCCOCCOCCOCCNC6=C(C(N(C7CCC(NC7=O)=O)C8=O)=O)C8=CC=C6)C=C5)=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.0829 mL5.4146 mL10.8292 mL
5 mM0.2166 mL1.0829 mL2.1658 mL
10 mM0.1083 mL0.5415 mL1.0829 mL
50 mM0.0217 mL0.1083 mL0.2166 mL

Description

ARV-825 is a Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.

Targets

BRD4 BD2 [1]
(Cell-free assay)
BRD4 BD1 [1]
(Cell-free assay)
28 nM(Kd)90 nM(Kd)

In vitro

Compared with the BRD4 inhibitors, ARV-825 treatment results in a strikingly more pronounced effect on the levels of c-MYC, and downstream cell proliferation and apoptosis induction in BL (Burkitt’s Lymphoma) cell lines.The IC50s of ARV-825 for all tested cell lines and primary AML cells at 72 hours are in the low nanomolar range (2-50 nM). ARV-825 treatment reduces PIM1 levels and phosphorylation of CXCR4 in AML cells while overexpression of PIM1 or Myc reverses the phenomena.