Entrectinib


CAS No. : 1108743-60-7

Entrectinib,1108743-60-7
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000440
Synonyms:(Z)-N-(5-(3,5-difluorobenzyl)-1H-indazol-3(2H)-ylidene)-4-(4-methylpiperazin-1-yl)-2-((tetrahydro-2H-pyran-4-yl)amino)benzamide
Molecular Formula:C₃₁H₃₄F₂N₆O₂
Molecular Weight:560.64
Target:ALK
IC50:1.7/0.1/0.1 nM (Trk A/B/C), 0.2 nM (ROS1), 1.6 nM (ALK)
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Appearance:Solid powder
Purity: > 98%
Cat No:I000440
Cas No:1108743-60-7
Product-Name:Entrectinib
InChI:InChI=1S/C31H34F2N6O2/c1-38-8-10-39(11-9-38)25-3-4-26(29(19-25)34-24-6-12-41-13-7-24)31(40)35-30-27-17-20(2-5-28(27)36-37-30)14-21-15-22(32)18-23(33)16-21/h2-5,15-19,24,34H,6-14H2,1H3,(H2,35,36,37,40)
InChIKey:HAYYBYPASCDWEQ-UHFFFAOYSA-N
SMILES:N1CCN(CC1)C2=CC(=C(C=C2)C(=O)NC3=NNC4=C3C=C(C=C4)CC5=CC(=CC(=C5)F)F)NC6CCOCC6

Entrectinib (RXDX-101) is an oral pan-Trk, ROS1, and ALK inhibitor, with IC50 of 1.7/0.1/0.1 nM, 0.2 nM, and 1.6 nM for Trk A/B/C, ROS1, and ALK, respectively.
RXDX-101 has demonstrated potent pharmacological activity in preclinical studies and has the potential to be first-in-class against the Trk family of kinases. PXDX-101 has been well tolerated in patients with advanced solid tumors. PXDX-101 is currently in clinical trials, and is being developed by Ignyta.


1. Expert Opin Investig Drugs. 2015;24(11):1493-500. doi: 10.1517/13543784.2015.1096344. Epub 2015 Oct 12.
Entrectinib: a potent new TRK, ROS1, and ALK inhibitor.
Rolfo C(1), Ruiz R(2), Giovannetti E(3), Gil-Bazo I(4), Russo A(5), Passiglia F(1)(5), Giallombardo M(1), Peeters M(1), Raez L(6).
Author information:
(1)a Phase I - Early Clinical Trials Unit, Oncology Department , Antwerp University Hospital and Center for Oncological Research (CORE), Antwerp University , Edegem , Belgium. (2)b Oncology Department , National Cancer Institute (INEN) , Lima , Peru. (3)c Department Medical Oncology , VU University Medical Center , Amsterdam , The Netherlands. (4)d Department of Oncology , Clínica Universidad de Navarra , Pamplona , Spain. (5)e Department of Surgical, Oncological and Oral Sciences, Section of Medical Oncology , University of Palermo , Palermo , Italy. (6)f Thoracic Oncology Program , Memorial Cancer Institute, Memorial Health Care System , Pembroke Pines , FL , USA.
INTRODUCTION: Receptor tyrosine kinases (RTKs) and their signaling pathways, control normal cellular processes; however, their deregulation play important roles in malignant transformation. In advanced non-small cell lung cancer (NSCLC), the recognition of oncogenic activation of specific RTKs, has led to the development of molecularly targeted agents that only benefit roughly 20% of patients. Entrectinib is a pan-TRK, ROS1 and ALK inhibitor that has shown potent anti-neoplastic activity and tolerability in various neoplastic conditions, particularly NSCLC.
AREAS COVERED: This review outlines the pharmacokinetics, pharmacodynamics, mechanism of action, safety, tolerability, pre-clinical studies and clinical trials of entrectinib, a promising novel agent for the treatment of advanced solid tumors with molecular alterations of Trk-A, B and C, ROS1 or ALK. EXPERT OPINION: Among the several experimental drugs under clinical development, entrectinib is emerging as an innovative and promising targeted agent. The encouraging antitumor activity reported in the Phase 1 studies, together with the acceptable toxicity profile, suggest that entrectinib, thanks to its peculiar mechanism of action, could play an important role in the treatment-strategies of multiple TRK-A, B, C, ROS1, and ALK- dependent solid tumors, including NSCLC and colorectal cancer. That being said, further evidence for its clinical use is still needed.
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