Entrectinib (RXDX-101) - Moligand™, 10mM in DMSO , ALK tyrosine kinase receptor inhibitor, CAS No.1108743-60-7, ALK tyrosine kinase receptor inhibitor

CAS: 1108743-60-7 Cat. No.: E407778 Summenformel: C₃₁H₃₄F₂N₆O₂ Molekulargewicht: 560.64 EG-Nummer: 816-298-8

QUALITÄT & REINHEIT Moligand™, 10mM in DMSO

Synonyms

NMS-E628 | N-(5-(3,5-difluorobenzyl)-1H-indazol-3-yl)-4-(4-methylpiperazin-1-yl)-2-(tetrahydro-2H-pyran-4-ylamino)benzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

Entrectinib (RXDX-101, NMS-E628) is an orally bioavailable pan-TrkA/B/C,ROS1andALKinhibitor withIC50ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) inducesautophagy. Phase 2.
In vitro

Entrectinib selectively blocks proliferation of ALK-dependent cell lines and potently inhibits ALK‐dependent signaling. Entrectinib also highly inhibits cell growth of the NSCLC cell line NCI‐H2228 bearing the EML4-ALK rearrangement.

In vivo

In mice bearing Karpas-299 and SR-786 xenografts, Entrectinib (p.o.) induces complete tumor regression. In NPM-ALK transgenic mice, Entrectinib induces complete regression of tumor masses observed in the thymus and in lymph nodes. In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy.
Cell Data

cell lines：Tumor cell lines including MDA-MB-361, MDA-MB-231, MDA-MB-468, LNCap, DU145, A498, and HCT116

Concentrations：

Incubation Time：

Powder Purity:≥97%

Spezifikationen

Synonyme

NMS-E628 | N-(5-(3,5-difluorobenzyl)-1H-indazol-3-yl)-4-(4-methylpiperazin-1-yl)-2-(tetrahydro-2H-pyran-4-ylamino)benzamide

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

Entrectinib (RXDX-101, NMS-E628) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

INHIBITOR

Mechanismus der Wirkung

ALK tyrosine kinase receptor inhibitor

Produkteigenschaften

ALogP

5.7

Namen und Kennungen

Isomere SMILES

CN1CCN(CC1)C2=CC(=C(C=C2)C(=O)NC3=NNC4=C3C=C(C=C4)CC5=CC(=CC(=C5)F)F)NC6CCOCC6

Molekulargewicht

560.64

Reaxy-Rn

18969663

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18969663&ln=

Zugehörige Ziele (menschlich)

ROS1 Tclin Proto-oncogene tyrosine-protein kinase ROS (3 Activities)

Discover Target: ROS1

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

FRK Tchem Tyrosine-protein kinase FRK (1 Activities)

Discover Target: FRK

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

FER Tclin Tyrosine-protein kinase Fer (1 Activities)

Discover Target: FER

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

LTK Tclin Leukocyte tyrosine kinase receptor (1 Activities)

Discover Target: LTK

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

ALK Tclin ALK tyrosine kinase receptor (5 Activities)

Discover Target: ALK

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

NTRK2 Tclin BDNF/NT-3 growth factors receptor (3 Activities)

Discover Target: NTRK2

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

NTRK1 Tclin High affinity nerve growth factor receptor (8 Activities)

Discover Target: NTRK1

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

NTRK3 Tclin NT-3 growth factor receptor (3 Activities)

Discover Target: NTRK3

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)

Chemische und physikalische Eigenschaften

• Löslichkeit: Solubility (25°C) In vitro DMSO: 70 mg/mL (201.27 mM); Ethanol: 7 mg/mL (20.12 mM); Water: Insoluble

Häufig gestellte Fragen

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

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 1108743-60-7, the molecular formula is C31H34F2N6O2, and the molecular weight is 560.64 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.