1341200-45-0 Usage
Uses
TP-0903 is an AXL kinase inhibitor.
Biological Activity
axl and other tam family members are known to be involved in maintaining the mesenchymal phenotype in cancer cells. mesenchymal cells have increased invasion and migratory properties, enhanced cell survival in stressed environments, as well as increased resistance to targeted therapies. tp-0903 is a potent anti-cancer agent targeting the axl receptor tyrosine kinase.
in vitro
on the basis of the potency of tp-0903 in biochemical assays, its activity in cell-based studies was evaluated. tp-0903 showed extremely potent activity in cell viability assays against the pancreatic cancer cell line psn-1. more importantly, tp-0903 was evaluated for its ability to block gas6-mediated activation of axl in pancreatic cancer cells. psn-1 cells were serum-starved and then stimulated with gas6 in the presence of various concentrations of tp-0903 [1].
in vivo
tp-0903 restores sensitivity to erlotinib in cell-based and preclinical animal models of cancer by reversing the mesenchymal phenotype driving resistance [2].
IC 50
0.027 μm against axl
references
[1] mollard a, warner sl, call lt, wade ml, bearss jj, verma a, sharma s, vankayalapati h, bearss dj. design, synthesis and biological evaluation of a series of novel axl kinase inhibitors. acs med chem lett. 2011 dec 8;2(12):907-912.[2] toleropharmaceuticals, inc–tp-0903. http://www.toleropharmaceuticals.com/tp-0903.html.
Check Digit Verification of cas no
The CAS Registry Mumber 1341200-45-0 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,4,1,2,0 and 0 respectively; the second part has 2 digits, 4 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 1341200-45:
(9*1)+(8*3)+(7*4)+(6*1)+(5*2)+(4*0)+(3*0)+(2*4)+(1*5)=90
90 % 10 = 0
So 1341200-45-0 is a valid CAS Registry Number.
1341200-45-0Relevant articles and documents
AXL INHIBITOR FORMULATIONS
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, (2021/04/10)
Formulations of Compound 1 or a pharmaceutically acceptable salt thereof are described. Also disclosed are capsules having a dry blended powder comprising Compound 1 or a pharmaceutically acceptable salt thereof. The Compound 1 or a pharmaceutically accep
AXL KINASE INHIBITORS AND USE OF THE SAME
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Page/Page column 162; 164, (2019/10/29)
Tartrate salts of the compound of structure (I), crystalline forms thereof, and therapeutic applications thereof for treating solid tumors (e.g., advanced solid tumor) or hematopoietic cancers. Also provided herein are methods for synthesizing the tartrat
Design, synthesis, and biological evaluation of a series of novel AXL kinase inhibitors
Mollard, Alexis,Warner, Steven L.,Call, Lee T.,Wade, Mark L.,Bearss, Jared J.,Verma, Anupam,Sharma, Sunil,Vankayalapati, Hariprasad,Bearss, David J.
supporting information; experimental part, p. 907 - 912 (2012/01/19)
The receptor tyrosine kinase AXL has emerged in recent years as an potential oncology target due to its overexpression in several types of cancers coupled with its ability to promote tumor growth and metastasis. To identify small molecule inhibitors of AXL, we built a homology model of its catalytic domain to virtually screen and identify scaffolds displaying an affinity for AXL. Further computational and structure-based design resulted in the synthesis of a series of 2,4,5-trisubstitued pyrimidines, which demonstrated potent inhibition of AXL in vitro (IC50 = 19 nM) and strongly inhibited the growth of several pancreatic cell lines.
