JNJ-7706621 - Moligand™, 10mM in DMSO , Inhibitor of aurora kinase A;Inhibitor of aurora kinase B;Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 2;Inhibitor of Janus kinase 2, CAS No.443797-96-4, Inhibitor of aurora kinase A;Inhibitor of aurora kinase B;Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 2;Inhibitor of Janus kinase 2

CAS: 443797-96-4 Cat. No.: J408880 Peso molecular: 394.36

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

4-​[[5-​amino-​1-​(2,​6-​difluorobenzoyl)​-​1H-​1,​2,​4-​triazol-​3-​yl]​amino]​-benzenesulfonamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

JNJ-7706621 is pan-CDKinhibitor with the highest potency on CDK1/2 withIC50of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
In vitro

JNJ-7706621 also shows some inhibition to VEGF-R2, FGF-R2, and GSK3β, with IC50 of 154-254 nM. JNJ-7706621 shows inhibitory effect on a panel of human cancer cell types, including HeLa, HCT-116, SK-OV-3, PC3, DU145, A375, MDA-MB-231, MES-SA, and MES-SA/Dx5, with IC50 of 112-514 nM, independent of p53, retinoblastoma, or P-glycoprotein status. JNJ-7706621 is several-fold less potent at inhibiting growth of normal cell types, including MRC-5, HASMC, HUVEC, and HMVEC, with IC50 of 3.67-5.42 μM. In HeLa or U937 cells, JNJ-7706621 (0.5-3 μM) delays exit from G1, arrests cells in G2-M, induces endoreduplication, activates apoptosis, and reduces colony formation. In a HeLa cell line, incremental treatment with increasing concentrations of JNJ-7706621 leads to a 16-fold resistance, which may be mediated by ABCG2.

In vivo

In mouse xenograft model of A375 melanoma human tumor, JNJ-7706621 (100 or 125 mg/kg) causes tumor regression.
Cell Data

cell lines：HepG2 Ntcp and Huh7-Ntcp cells

Concentrations：1 nM - 10 μM, dissolved in DMSO

Incubation Time：48 hours

Powder Purity:≥97%

Specifications

Sinónimos

4-​[[5-​amino-​1-​(2, ​6-​difluorobenzoyl)​-​1H-​1, ​2, ​4-​triazol-​3-​yl]​amino]​-benzenesulfonamide

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of aurora kinase A;Inhibitor of aurora kinase B;Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 2;Inhibitor of Janus kinase 2

Nombres e identificadores

• Isómeros SMILES: C1=CC(=C(C(=C1)F)C(=O)N2C(=NC(=N2)NC3=CC=C(C=C3)S(=O)(=O)N)N)F
• Peso molecular: 394.36
• Reaxy-Rn: 10202230
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10202230&ln=

Objetivos asociados (humanos)

CDK1 Tchem Cyclin-dependent kinase 1 (2 Activities)

Discover Target: CDK1

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

CDK9 Tchem Cyclin-dependent kinase 9 (1 Activities)

Discover Target: CDK9

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

CDK16 Tchem Cyclin-dependent kinase 16 (1 Activities)

Discover Target: CDK16

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

CDK2 Tchem Cyclin-dependent kinase 2 (3 Activities)

Discover Target: CDK2

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

CDK5 Tchem Cyclin-dependent-like kinase 5 (2 Activities)

Discover Target: CDK5

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

TAOK1 Tchem Serine/threonine-protein kinase TAO1 (1 Activities)

Discover Target: TAOK1

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

JAK1 Tclin Tyrosine-protein kinase JAK1 (3 Activities)

Discover Target: JAK1

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

AURKA Tchem Aurora kinase A (2 Activities)

Discover Target: AURKA

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

AURKB Tchem Aurora kinase B (2 Activities)

Discover Target: AURKB

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

NUAK2 Tchem NUAK family SNF1-like kinase 2 (1 Activities)

Discover Target: NUAK2

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

JAK2 Tclin Tyrosine-protein kinase JAK2 (1 Activities)

Discover Target: JAK2

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

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 3.1 mg/mL warmed with 50ºC Water: bath (9.87 mM); Water: Insoluble; Ethanol: Insoluble