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Entrectinib

Description Effect and benefit Mechanism of action Safety Pharmacology
Entrectinib
Entrectinib structure
CAS No.
1108743-60-7
Chemical Name:
Entrectinib
Synonyms
CS-1589;NMS-E628;RXDX-101;Entrectinib;entrecitinib;Entrectinib(NMS-E628);Entrectinib(RXDX-101);Entrectinib,NMS-E628,RXDX-101;NMS E628; RXDX-101;NMSE628; RXDX 101;NMS-E628; RXDX101;RXDX101; RXDX 101; RXDX-101; NMS E628; NMSE628; NMS-E628; ENTRECTINIB
CBNumber:
CB93040787
Molecular Formula:
C31H34F2N6O2
Formula Weight:
560.64
MOL File:
1108743-60-7.mol

Entrectinib Properties

Boiling point:
717.5±60.0 °C(Predicted)
Density 
1.340±0.06 g/cm3(Predicted)
pka
12.01±0.43(Predicted)
FDA UNII
L5ORF0AN1I
NCI Dictionary of Cancer Terms
entrectinib
NCI Drug Dictionary
entrectinib

Entrectinib price More Price(3)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 19476 Entrectinib ≥98% 1108743-60-7 1mg $28 2021-03-22 Buy
Cayman Chemical 19476 Entrectinib ≥98% 1108743-60-7 5mg $98 2021-03-22 Buy
Cayman Chemical 19476 Entrectinib ≥98% 1108743-60-7 10mg $182 2021-03-22 Buy

Entrectinib Chemical Properties,Uses,Production

Description

Entrectinib is used to treat metastatic (lung cancer that has already spread) non-small cell lung cancer (NSCLC) that is caused by a gene called ROS1. This medicine is also used to treat solid tumors (cancer) that are caused by certain abnormal NTRK genes and have spread or if surgery to remove the cancer is likely to cause severe complications, and there is no acceptable treatment option or the cancer grew or spread on other treatments.

Effect and benefit

Entrectinib belongs to the group of medicines called antineoplastics (cancer medicines). It works by interfering with the growth of cancer cells, which are eventually destroyed.

Mechanism of action

An inhibitor of tropomyosin receptor tyrosine kinases (TRKs) TRKA, TRKB, and TRKC (encoded by the neurotrophic tyrosine receptor kinase [NTRK] genes NTRK1, NTRK2, and NTRK3, respectively), proto-oncogene tyrosine-protein kinase ROS1 (ROS1), and anaplastic lymphoma kinase (ALK); also, inhibits JAK2 and TNK2. Major active metabolite of entrectinib, M5, showed similar in vitro activity against TRK, ROS1, and ALK. Fusion proteins that include TRK, ROS1, or ALK kinase domains can drive tumorigenic potential through hyperactivation of downstream signaling pathways, leading to unconstrained cell proliferation.

Safety

Entrectinib exhibits hepatic metabolism through cytochrome P450 (CYP) 3A and therefore interacts with moderate-strong CYP3A inhibitors and inducers. In addition, due to its effects on the QTcF interval, use of entrectinib should be avoided with other drugs known to prolong the QT/QTc interval.

Pharmacology

Entrectinib, is a weak P-gp substrate that can sustain CNS exposure based on our novel in vitro and in vivo experiments. This is consistent with the observed preclinical and clinical efficacy of entrectinib in neurotrophic tropomyosin receptor kinase (NTRK) and ROS1 fusion-positive CNS tumors and secondary CNS metastases.

Description

Entrectinib (RXDX-101, Ignyta Pharmaceuticals, San Diego, CA, USA) is a small molecule that inhibits the tyrosine kinases TRKA/B/C, ROS1, and ALK (Table?1). It has a preclinical median inhibitory concentration (IC50) of 7?nm against ROS1, higher than crizotinib [95, 96]. Entrectinib was specifically designed to cross the blood-brain barrier [95].

Clinical Use

Entrectinib demonstrated potent antitumor effects in tumor cell lines and patient-derived xenograft (PDX) tumor models in preclinical studies. Furthermore, entrectinib can cross the blood–brain barrier (BBB) to impact primary brain tumors and brain metastases in patients with NTRK1/ NTRK2/NTRK3, ROS1, and ALK fusion-driven cancers.

Entrectinib Preparation Products And Raw materials

Raw materials

Preparation Products


Entrectinib Suppliers

Global( 129)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Shanghai Payne Pharmaceutical Technology Co.Ltd
18678586262 021-58123769
info@paynepharm.com China 1355 58
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26734 60
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29959 58
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
+86-755-23284190 sales@tianpharm.com CHINA 305 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 968 58
BOC Sciences
1-631-485-4226
1-631-614-7828 inquiry@bocsci.com United States 19753 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 37282 58
Alchem Pharmtech,Inc.
8485655694
sales@alchempharmtech.com United States 63726 58
Zhuozhou Wenxi import and Export Co., Ltd
+8613111626072 (WhatsApp)
Wechat: +8613111626072 Wickr me: waynehu zzwenxi@126.com CHINA 13187 58
Target Molecule Corp
18019718960 781-999-5354
marketing@targetmol.com United States 19232 58

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View Lastest Price from Entrectinib manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-10-08 Entrectinib
1108743-60-7
US $0.00-0.00 / g 1g 98% 100kgs Wuhan Nutra Biotechnology Co.,Ltd
2021-07-13 BMN 673
1108743-60-7
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd
2021-07-10 BMN 673
1108743-60-7
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd

1108743-60-7(Entrectinib)Related Search:


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  • API
  • API
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