Lorlatinib ( PF -06463922) ; CAS1454846-35-5

Colour
White
Shelf Life
2-3 Years
Lead Time
5-7 Working Days
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MOQ
10g
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ISO9001/SGS
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in Stock
Package
1kg/5kg/10kg/25kg
Purity
99%
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Drum/Bottle/Bags
Trademark
Yunbang
Origin
China
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Product Description

Lorlatinib (PF-06463922);CAS 1454846-35-5
 
Lorlatinib (PF-06463922) ; CAS1454846-35-5
Lorlatinib (PF-06463922) Chemical Properties
Boiling point  675.0±55.0 °C(Predicted)
density  1.42±0.1 g/cm3(Predicted)
pka 6.05±0.40(Predicted)
CAS DataBase Reference 1454846-35-5
 
Safety Information
 
MSDS Information
 
 
Lorlatinib (PF-06463922) Usage And Synthesis
Description Lorlatinib (PF-06463922) is a new drug under development for the sub-group of advanced non-small cell lung cancerwho are ALK or ROS1 positive and have already undergone gene treatment with drugs thatspecifically targetthis type of cancer.Lorlatinib is currently being evaluated in phase II clinical trials as an oral dose at 100 mg daily. If marketed it will becomean additional targeted treatment for this sub-group of ALKor ROS1 positive patients.
Lorlatinib acts by inhibiting the ALK and ROS1 receptor tyrosine kinases, with potent activity against a broad spectrum of ALK resistant mutations. By inhibiting ALK phosphorylation and ROS1 activity, lorlatinib inhibits the downstream signalling, thereby inducing the apoptosis process, which results in the inhibition of tumour cells proliferation.
Due to tumor complexity and development of resistance to treatment, disease progression is a challenge in patients with ALK-positive metastatic non-small cell lung cancer (NSCLC). A common site for progression in metastatic NSCLC is the brain.
Lorlatinib was specifically designed to inhibit tumor mutations that drive resistance to other ALK inhibitors and to penetrate the blood brain barrier.
Mechanism of Action Lorlatinib is a kinase inhibitor with in vitro activity against ALK and number of other tyrosine kinase receptor related targets including ROS1, TYK1, FER, FPS, TRKA, TRKB, TRKC, FAK, FAK2, and ACK Label. Lorlatinib demonstrated in vitro activity against multiple mutant forms of the ALK enzyme, including some mutations detected in tumors at the time of disease progression on crizotinib and other ALK inhibitors Label. Moreover, lorlatinib possesses the capability to cross the blood-brain barrier, allowing it to reach and treat progressive or worsening brain metastases as well. The overall antitumor activity of lorlatinib in in-vivo models appears to be dose-dependent and correlated with the inhibition of ALK phosphorylation Label.
Although many ALK-positive metastatic NSCLC patients respond to initial tyrosine kinase therapies, such patients also often experience tumor progression. Various clinical trials performed with lorlatinib, however, have demonstrated its utility to effect tumor regression in ALK-positive metastatic NSCLC patients who experience tumor progression despite current use or having already used various first and second-generation tyrosine kinase inhibitors like crizotinib, alectinib, or ceritinib.
Uses Lorlatinib is a selective tyrosine kinase receptor inhibitor used in the therapy of selected cases of advanced non-small cell lung cancer.Lorlatinib has been used in trials studying the basic science and treatment of Non-small Cell Lung Cancer and anaplastic lymphoma kinase (ALK)-positive Non-Small Cell Lung Cancer (NSCLC) and ROS1-positive NSCLC. Despite initial responses from the use of various ALK inhibitors, however, it is virtually almost guaranteed that all patients with the condition in question will develop tumour progression or resistance to the current therapy in use.
Side effects A third-generation ALK- and ROS1-inhibitor, lorlatinib, has demonstrated activity following progression on one or more ALK inhibitors.Lorlatinib is approved for ALK-positive NSCLC. Similar to other agents in this category, lorlatinib is associated with hepatotoxicity and interstitial lung disease/pneumonitis. CNS toxicities, hyperlipidemia, and atrioventricular block have also been reported.
Uses Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase that promotes cell proliferation and blocks apoptosis. PF-06463922 is an ATP-competitive, selective inhibitor of ALK (Ki = < 0.07 nM) and c-Ros oncogene 1 (ROS1, Ki = 0.7 nM). It has strong activity against all known ALK and ROS1 mutants identified in patients, including the EML4-L1196M mutant of ALK (Ki = < 0.02 nM). PF-06463922 is orally available, displaying inhibition of ALK phosphorylation and antitumor efficacy in a xenograft model expressing EML4-L1196M ALK. It demonstrates efficient blood-brain barrier penetration, produces brain tumor regression in mice harboring EML4-ALK tumors, and increases overall survival.[Cayman Chemical]
Enzyme inhibitor This potent, dual ALK/ROS1 inhibitor (FW = 406.41 g/mol; CAS 1454846- 35-5), also named (10R)-7-amino-12-fluoro-10,15,16,17-tetrahydro- 2,10,16-trimethyl-15-oxo-2H-4,8-methenopyrazolo[4,3- h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile, targets the protooncogene tyrosine-protein kinase ROS1 (Ki < 0.02 nM) as well as wild-type anaplastic lymphoma kinase ALKWT (Ki < 0.07 nM) and its Leu-to-Met mutant ALKL1196M (Ki of = 0.7 nM). PF-06463922 significantly inhibits cell proliferation and induces cell apoptosis in the HCC78 human NSCLC cells harboring SLC34A2-ROS1 fusions and the BaF3-CD74-ROS1 cells expressing human CD74-ROS1
 
Lorlatinib (PF-06463922) ; CAS1454846-35-5
 
Lorlatinib (PF-06463922) ; CAS1454846-35-5 Lorlatinib (PF-06463922) ; CAS1454846-35-5 Lorlatinib (PF-06463922) ; CAS1454846-35-5
Company Informations:

Hunan Yunbang Pharmaceutical Co., Ltd. ( Yunbangpharm) located in Changsha High-tech Industrial Park, Hunan. It is a high-tech enterprise specializing in the research and development, production and sales of Pharmaceutical raw materials, Pharmaceutical intermediates(API) and Fine chemicals. Based in China, Yunbangpharm has been providing suitable solutions for many domestic,foreign pharmaceutical companies and traders. Excellent quality, good reputation and authentic price have won the praise of the majority of customers.
The company adheres to the corporate tenet of "We do not produce medicines, but help pharmaceutical companies make good medicines".

We can provide customers with customized processing, research and development services;
We can develop high-end Pharmaceutical and chemical products with high technical difficulties,high barriers and unique production processes;
We can provide 100 grams Grade, kilograms, and hundred kilograms of raw material pharmaceutical intermediates and other products.
We can perform -100°C to 300°C reaction.

R&D strength is the company's core competitiveness.Yunbangpharm has maintains a good cooperation relationship with many Universities and Research institutes locally, which can quickly transform R&D results into industrial production.

Our goal : To achieve the integrated upgrade of P harmaceutical intermediates, raw materials and high-end chemical products, adhere to "serving pharmaceutical companies, creating our brands" to provide customers with high-quality and low-cost pharmaceutical and chemical products, realizing Win-win cooperation and common development.

 

Organic Intermediate

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