Conteltinib - 10mM in DMSO , CAS No.1384860-29-0

CAS: 1384860-29-0 Cat. No.: C654599 Fórmula: C₃₂H₄₅N₉O₃S Peso molecular: 635.82 PubChem CID: 89860551

GRAU & PUREZA 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK , ALK, and Pyk2 . Conteltinib exerts significant inhibitory effect on FAK with an IC 50 of 1.6 nM

In Vitro

Conteltinib (CT-707) synergizes with XL184 to suppress hepatocellular carcinoma by blocking XL184-induced FAK activation. ?\nThe combination of XL184 (5 μM) and Conteltinib (3 μM) significantly reduces the survival fraction, compared with each agent alone. ?\nThe combination of XL184 (5 μM) and Conteltinib (3 μM) results in enhanced caspase-dependent apoptosis in human hepatocellular carcinoma cell lines. ?\nThe FAK phosphorylation induced by XL184 (5 μM) might be involved in the synergistic antitumor effect of Conteltinib (3 μM) and XL184. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: The human hepatocellular carcinoma cell lines HepG2 and Bel-7402 Concentration: 1.0, 1.5, 2.0, 2.5, and 3.0 μM for HepG2 cells; 0.2, 0.4, 0.8, 1.5, and 3.0 μM for Bel-7402 cells Incubation Time: 72 hours Result: When cells were exposed to XL184 (5 μM), Conteltinib (3 μM), or their combination, the survival rates were 57.3%, 39.3%, and 11.2%, respectively, in HepG2; those in Bel-7402 were 57.8%, 61.6%, and 34.2%, respectively. Apoptosis AnalysisCell Line: HepG2 and Bel-7402 cells Concentration: 3 μM Incubation Time: 48 hours Result: The apoptosis rates of control, XL184, Conteltinib, and combination groups in HepG2 were 5.0%, 10.5%, 18.4%, and 41.1%, respectively, and those in Bel-7402 were 4.4%, 16.3%, 8.7%, and 36.4%, respectively. Western Blot AnalysisCell Line: HepG2 and Bel-7402 Concentration: 3 μM Incubation Time: 24 hours Result: Could markedly decrease FAK phosphorylation induced by XL184, which might partially account for the synergetic effect.

In Vivo

The combination of XL184? (20 mg/kg once daily for first 3 days; i.g. 10 mg/kg once a day for 4th day; no administration from 5th to 10th days; i.g. 10 mg/kg once a day from the 10th to 14th days )and CT-707? (i.g. 50 mg/kg twice a day for first 3 days, 7th, 8th, 11th, 12th, and 14th days; once a day for 4th, 6th, 9th, 10th, and 13th days; no administration for the 5th day) shows? the synergistic antitumor effect in HepG2 xenograft nude mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice transplanted with HepG2 xenografts Dosage: 50 mg/kg Administration: Intragastrically (i.g.) twice a day for first 3 days, 7th, 8th, 11th, 12th, and 14th days; once a day for 4th, 6th, 9th, 10th, and 13th days; no administration for the 5th day. Result: Caused a moderate decrease in the relative tumor volume (RTV). The inhibition rate of combination group reached 77.4%, whereas the mono-treatment of XL184 or CT-707 alone caused 30.7% and 19.4% inhibition in the tumor weight, respectively.

IC50& Target:IC50: 1.6 nM (FAK)

Especificações

Especificações e pureza

10mM in DMSO

Mecanismos bioquímicos e fisiológicos

Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK , ALK, and Pyk2 . Conteltinib exerts significant inhibitory effect on FAK with an IC 50 of 1.6 nM.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

INHIBITOR

Propriedades do produto

ALogP

5.1

Nomes e identificadores

SMILES isoméricas

CC(C)NS(=O)(=O)C1=CC=CC=C1NC2=NC(=NC3=C2CCN3)NC4=C(C=C(C=C4)N5CCC(CC5)N6CCN(CC6)C)OC

CAS alternativo

1384860-29-0

PubChem CID

89860551

Termos de entrada MeSH

2-((2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)anilino)-6,7-dihydro-5H-pyrrolo(2,3-d)pyrimidin-4-yl)amino)-N-(propan-2-yl)benzene-1-sulfonamide;conteltinib;CT-707

Peso molecular

635.82

Alvos associados (humanos)

PTK2 Tclin Focal adhesion kinase 1 (0 Activities)

Discover Target: PTK2

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

PTK2B Tclin Protein-tyrosine kinase 2-beta (0 Activities)

Discover Target: PTK2B

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

Perguntas frequentes

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

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 1384860-29-0, the molecular formula is C32H45N9O3S, and the molecular weight is 635.82 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.