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 Molecular Weight: 560.64 EC Number: 816-298-8
AVAILABLE TO ORDER
GRADE & PURITY Moligand™ ? Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools. 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
 ·  off list, applied to all prices below.
Size
Status
Price
Qty
1ml
E407778-1ml
2

$296.90

$432.90
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Why this grade

Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.

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Storage & shipping

Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.

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Quality documents

SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.

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Literature proof

Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.

Overview

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%

Specifications

Synonyms
NMS-E628 | N-(5-(3, 5-difluorobenzyl)-1H-indazol-3-yl)-4-(4-methylpiperazin-1-yl)-2-(tetrahydro-2H-pyran-4-ylamino)benzamide
Specifications & Purity
Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms
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
Shipped In
Dry ice packs + Cold packs
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
ALK tyrosine kinase receptor inhibitor
Product Properties
ALogP5.7
Names and Identifiers
Isomeric SMILES CN1CCN(CC1)C2=CC(=C(C=C2)C(=O)NC3=NNC4=C3C=C(C=C4)CC5=CC(=CC(=C5)F)F)NC6CCOCC6
Molecular Weight 560.64
Reaxy-Rn 18969663
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18969663&ln=

Documentation

📋 Safety Data Sheet (SDS)

Comprehensive hazard, handling, storage, and regulatory compliance document.

Download SDS →

✅ Certificate of Analysis (COA)

Lot-specific quality data. Enter your lot number to retrieve the exact COA.

Look up COA →

📊 Datasheet

Quick-reference summary of product specifications and applications.

View datasheet →

🔬 Specification Sheet

Full quality attributes and acceptance criteria for this grade.

View spec sheet →

Advanced Data

Associated Targets(Human)
ROS1 Tclin Proto-oncogene tyrosine-protein kinase ROS (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FRK Tchem Tyrosine-protein kinase FRK (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FER Tclin Tyrosine-protein kinase Fer (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
LTK Tclin Leukocyte tyrosine kinase receptor (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ALK Tclin ALK tyrosine kinase receptor (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
NTRK2 Tclin BDNF/NT-3 growth factors receptor (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
NTRK1 Tclin High affinity nerve growth factor receptor (8 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
NTRK3 Tclin NT-3 growth factor receptor (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK2 Tclin Tyrosine-protein kinase JAK2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
Certificates(CoA,COO,BSE/TSE and Analysis Chart)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Chemical and Physical Properties
SolubilitySolubility (25°C) In vitro DMSO: 70 mg/mL (201.27 mM); Ethanol: 7 mg/mL (20.12 mM); Water: Insoluble;
Solution Calculators
Reviews

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