A1874|BRD4-degrading PROTAC|2064292-12-0

Cas No.:	2064292-12-0
Chemical Name:	(2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-N-(4-((1-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-2-oxo-6,9,12-trioxa-3-azatetradecan-14-yl)carbamoyl)-2-methoxyphenyl)-4-cyano-
Synonyms:	A-1874,A 1874
SMILES:	N1[C@H](CC(C)(C)C)[C@](C2=CC=C(Cl)C=C2F)(C#N)[C@H](C2=CC=CC(Cl)=C2F)[C@H]1C(NC1=CC=C(C(=O)NCCOCCOCCOCCNC(=O)C[C@H]2N=C(C3=CC=C(Cl)C=C3)C3C(C)=C(C)SC=3N3C(C)=NN=C32)C=C1OC)=O
Formula:	C₅₈H₆₂Cl₃F₂N₉O₇S
M.Wt:	1173.597
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation[1].

In Vitro:

Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) induces a dose-dependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nmol/L and a maximum degradation (Dmax) of BRD4 of 98% of the levels in control (0.1% DMSO-treated) cells[1]. Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) increases p53 levels in the HCT116 cells and showed dose-dependent p53 stabilization[1]. Western Blot Analysis[1] Cell Line: HCT116 cells. Concentration: 0-10 μM. Incubation Time: 24 hours. Result: Induced a dosedependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nM.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC26169	MS1943	MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines.
DC21360	MZ1	MZ1 is a PROTAC that tethers JQ1 to a ligand for the E3 ubiquitin ligase VHL, triggers, induces degradation of the BET bromodomain BRD4.
DC21351	MS4078	MS4078 is a novel PROTAC (degrader) of ALK, potently decreases cellular levels of oncogenic active ALK fusion proteins in a concentration- and time-dependent manner in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells (DC50=11 nM).
DC20367	dTRIM24	dTRIM24 is a potent TRIM24 bromodomain inhibitor with IC50 of 217.8 nM (TRIM24 ligand displacement).
DC21893	dBET57	dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=500 nM), but is inactive on BRD4 BD2..
DC12702	A1874	A1874 (A-1874) is a nutlin-based and BRD4-degrading PROTAC with DC50 of 32 nM (induce BRD4 degradation in cells).