CF53 - 10mM in DMSO , CAS No.1808160-52-2

CAS: 1808160-52-2 Cat. No.: C654650 분자식: C₂₄H₂₅N₇O₂ 분자량: 443.50 PubChem CID: 118340554

등급 & 순도 10mM in DMSO

Storage

Argon charged,Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K i of <1 nM, K d of 2.2 nM and an IC 50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2 , BRD3 , BRD4 , and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo

In Vitro

CF53 (Compound 28) binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, K d s are 1.1 nM (BRD2 BD1), 0.6 nM (BRD2 BD2), 0.52 nM (BRD3 BD1), 0.49 nM (BRD3 BD2), 0.8 nM (BRD4 BD2), 2 nM (BRDT BD1), 2.1 nM (BRDT BD2), 47 nM (CREBBP), 570 nM (CECR2), 110 nM (EP300), respectively. CF53 exhibits IC 50 s of 7, 85 nM against MOLM-13 acute leukemia and MDA-MB-231 breast cancer cell lines, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CF53 (25, 50 mg/kg, p.o.) exhibits potent anti-tumor activity both in MDA-MB-231 xenograft tumor model and in RS4;11 model in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:BRD4 (BD1) <1 nM (Ki) BRD4 (BD1) 2 nM (IC 50 ) BRD4 (BD1) 2.2 nM (Kd) BRD4 (BD2) 0.8 nM (Kd) BRD2 (BD2) 0.6 nM (Kd) BRD2 (BD1) 1.1 nM (Kd) BRD3 (BD2) 0.49 nM (Kd) BRD3 (BD1) 0.52 nM (Kd) BRDT (BD2) 1 nM (Kd) BRDT (BD1) 2 nM (Kd) CECR2 570 nM (Kd)

사양

사양 및 순도

10mM in DMSO

생화학 및 생리적 메커니즘

CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K i of <1 nM, K d of 2.2 nM and an IC 50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2 , BRD3 , BRD4 , and BRDT BET proteins with high affinit

보관 조건

Argon charged,Store at -80°C

배송

Dry ice packs + Cold packs

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작업 유형

INHIBITOR

이름과 식별자

이성체 SMILES

CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)NC4=C3C(=NC(=N4)C)NC5=CC(=NN5C)C6CC6)OC

PubChem CID

118340554

MeSH 용어

BET inhibitor CF53;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

분자량

443.50

관련 대상(인간)

EP300 Tchem Histone acetyltransferase p300 (1 Activities)

Discover Target: EP300

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CREBBP Tchem CREB-binding protein (1 Activities)

Discover Target: CREBBP

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 (3 Activities)

Discover Target: BRD4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CECR2 Tchem Cat eye syndrome critical region protein 2 (1 Activities)

Discover Target: CECR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRDT Tchem Bromodomain testis-specific protein (2 Activities)

Discover Target: BRDT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRD3 Tchem Bromodomain-containing protein 3 (2 Activities)

Discover Target: BRD3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRD2 Tchem Bromodomain-containing protein 2 (2 Activities)

Discover Target: BRD2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

자주 묻는 질문

How should this product be stored?

Store at ?80 °C under argon. It is supplied under an argon blanket; reseal under inert gas after each use.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1808160-52-2, the molecular formula is C24H25N7O2, and the molecular weight is 443.50 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.