1197958-12-5 AP26113

Superiority:

Product Name: AP26113
Synonyms: 5-chloro-2-N-[4-[4-(dimethylamino)piperidin-1-yl]-2-methoxyphenyl]-4-N-(2-dimethylphosphorylphenyl)pyrimidine-2,4-diamine;(2-((5-Chloro-2-((4-(4-(dimethylamino)piperidin-1-yl)-2-methoxyphenyl)amino)pyrimidin-4-yl)ami;AP26113;AP26113/AP-26113;5-chloro-N2-(4-(4-(diMethylaMino)piperidin-1-yl)-2-Methoxy-5-Methylphenyl)-N4-(2-(diMethylphosphoryl)phenyl)pyriMidine-2,4-diaMine;5-Chloro-N2-[4-[4-(dimethylamino)-1-piperidinyl]-2-methoxyphenyl]-N4-[2-(dimethylphosphinyl)phenyl]-2,4-pyrimidinediamine;(2-((5-chloro-2-((4-(4-(dimethylamino)piperidin-1-yl)-2-methoxyphenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide;AP26113-analog (ALK-IN-1)
CAS: 1197958-12-5
MF: C27H36ClN6O4P
MW: 575.039301
EINECS:
Product Categories: API;Inhibitors
Mol File: 1197958-12-5.mol

AP26113 Chemical Properties
Boiling point  737.6±70.0 °C(Predicted)
density  1.29±0.1 g/cm3(Predicted)
pka 9.27±0.20(Predicted)
CAS DataBase Reference 1197958-12-5

AP26113 Usage And Synthesis
Description AP26113 (also known as Brigatinib) is an investigated small molecule for targeted cancer therapy. It is a potent dual inhibitor of anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR). It is mainly under investigation for its treatmentefficacy on non-small cell lung cancer (NSCLC) where ALK is activated and EGFP mutations frequently occur.
Biological activity AP26113 is a kind of effective ALK inhibitor with an IC50 of 0.62 nM, being able to overcome the L1196M mutation-mediated Crizotinib resistance; Phase 2.
In vitro study AP26113 is highly effective in treating the sensitive-type and resistant-type H3122 cells, being able to reduce cell growth, inhibit the ALK phosphorylation and induce the apoptosis. This effect is in a dose-dependent manner. AP26113 acts on the H3122 and H3122 CR cells, reducing p-ALK with an IC50 of 7.4 and 16.8 nM, respectively. AP26113 acts on Ba/F3 cells expressing wild-type or mutant EML4-ALK, reducing the number of cells with an IC50 of 10 nM and 24 nM, respectively. AP26113 inhibits the growth of SU-DHL-1, H3122 and Ba/F3-EML4-ALK v1 cell lines with GI50 values of 9 nM, 4 nM and 13 nM, respectively. AP26113 acts on Karpas-299, SU-DHL-1 and L-82 cell lines through inhibiting ALK phosphorylation with an IC50 of 3.2 nM, 1.5 nM and 2.1 nM, respectively. AP26113 acts on Karpas-299 and H3122 cells and inhibits ALK and ERK phosphorylation in a dose-dependent manner. AP26113 acts on Ba/F3 cell lines (including wild-type EML4-ALK) and Ba/F3 cell lines (containing mutant EML4-ALK G1269S) and inhibits cell growth with an IC50 of 11 nM and 16 nM, respectively. AP26113 acts on Ba/F3 cell line (including wild-type EML4-ALK) and Ba/F3 cell line (containing mutant EML4-ALK E1210K), inhibits cell growth and inhibits ALK phosphorylation with IC50 of 74 nM and 335 nM, respectively. AP26113 (10 mg/kg-75 mg/kg) was effective in the EML4-ALK mutant mouse model of anti-PF-02341066.
AP26113 acts on the tumor expressing wild-type EMLA-ALK, or with G1269S and L1196M mutation, inducing the tumor regression. AP26113 acts on EGFR-DEL-expressing Ba/F3 cells and inhibits EGFR phosphorylation and activation with an IC50 of 75 nM and 114 nM, respectively. AP26113 acts on Ba/F3 cells expressing EGFR-DEL/T790M and inhibits EGFR phosphorylation and viability with the IC50 of 15 and 281 nM, respectively. AP26113 acts on the NSCLC cell line expressing EGFR-DEL (HCC827), inhibits EGFR phosphorylation. It has an IC50 of 62 nM, and inhibits cell growth as well with a GI50 of 165 nM. AP26113 acts on the HCC827 cell line expressing EGFR-DEL/T790M, inhibits EGFR phosphorylation with an IC50 of 59 nM and inhibits cell growth with a GI50 of 245 nM. AP26113 acts on HCC78 NSCLC cells and inhibits the signaling and proliferation of SLC34A2-ROS in a dose-dependent manner.