BET inhibitor CF53|

Cas No.:	1808160-52-2
Chemical Name:	N-(3-Cyclopropyl-1-methyl-1H-pyrazol-5-yl)-7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-2-methyl-9H-pyrimido[4,5-b]indol-4-amine
SMILES:	N1C2=C(C=C(OC)C(C3=C(C)ON=C3C)=C2)C2=C(NC3N(C)N=C(C4CC4)C=3)N=C(C)N=C12
Formula:	C₂₄H₂₅N₇O₂
M.Wt:	443.511
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

BET inhibitor CF53 is a highly potent, orally active inhibitor of bromodomain and extra-terminal (BET) with Ki of <1 nM (BRD4 BD1); potently inhibits different BET proteins with Kd values of 0.5-2.2 nM, weakly inhibits CREBBP (Ki=47 nM) and shows excellent selectivity over other bromodomain containing proteins; inhibits cell growth in MOLM-13 and MDA-MB-231 cell lines with IC50 of 7 and 85 nM, respectively; CF53 demonstrates significant antitumor activity in both triple-negative breast cancer and acute leukemia xenograft models in mice.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC10190	TPOP146	TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
DC11041	QCA276	QCA276 is a novel potent BET proteins inhibitor with IC50/Ki of 10/.3 nM, QCA276 is the BET ligand for PROTAC QCA570.
DC12248	PROTAC BET degrader-2	PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
DC11063	MS645	MS645 (MS-645) is a novel, bivalent bromodomain (BRD) inhibitor with Ki of 18.4 nM for tandem BD1-BD2 (BRD4 BD1/BD2 ), shows12- to 28-fold gain in affinity for binding to the tandem BD1-BD2 over the single BD1 or BD2.
DC12313	GNE-371	GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like, with an IC50 of 10 nM for TAF1(2).
DC9934	GNE-272	GNE-272 is a in Vivo Probe for the Bromodomains of CBP/EP300.
DC8556	BET-BAY 002	BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model.
DC11042	BET inhibitor CF53	BET inhibitor CF53 is a highly potent, orally active inhibitor of bromodomain and extra-terminal (BET) with Ki of <1 nM (BRD4 BD1).
DC7854	BAZ2-ICR	BAZ2-ICR is a selective BAZ2 bromodomain inhibitor (Kd values are 109 and 170 nM for BAZ2A and BAZ2B respectively).
DC11568	HJB-97	A potent BET bromodomian inhibitor with IC50 of 3-7 nM for BRD2/3/4 BD1 and BD2..