Afatinib is an effective first-line treatment for patients with EGFR-mutant NSCLC. Research groups designed and synthesized afatinib analogs to increase the inhibitory effect against EGFR and VEGFR2/KDR kinases. Meo. OMe HN HN OMe Afatinib Compound I Compound II The researchers run a series of tests to explore the kinase inhibitory activity of Afatinib and Compound I with EGFR. They found the IC50 of Compound I is 3.6 nM and that of Afatinib is 1.6nM. a. Please briefly explain the effectiveness of Compound I compare to Afatinib based on the information given
Afatinib is an effective first-line treatment for patients with EGFR-mutant NSCLC. Research groups designed and synthesized afatinib analogs to increase the inhibitory effect against EGFR and VEGFR2/KDR kinases. Meo. OMe HN HN OMe Afatinib Compound I Compound II The researchers run a series of tests to explore the kinase inhibitory activity of Afatinib and Compound I with EGFR. They found the IC50 of Compound I is 3.6 nM and that of Afatinib is 1.6nM. a. Please briefly explain the effectiveness of Compound I compare to Afatinib based on the information given
Biochemistry
9th Edition
ISBN:9781319114671
Author:Lubert Stryer, Jeremy M. Berg, John L. Tymoczko, Gregory J. Gatto Jr.
Publisher:Lubert Stryer, Jeremy M. Berg, John L. Tymoczko, Gregory J. Gatto Jr.
Chapter1: Biochemistry: An Evolving Science
Section: Chapter Questions
Problem 1P
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IC 50
The half maximal inhibitory concentration (IC50 ) is the concentration of a drug required to exert half the maximum inhibitory capacity of the drug. For example, here IC50 value of the drug afatinib is the amount of afatinib required to inhibit 50 percentage of EGFR and VEGFR2/KDR kinases
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