5-chloro-2-N-[4-[4-(dimethylamino)piperidin-1-yl]-2-methoxyphen-yl]-4-N-(2-dimethylphosphorylphenyl) CAS 1197958-12-5

Product Description:

5-chloro-2-N-[4-[4-(dimethylamino)piperidin-1-yl]-2-methoxyphen-yl]-4-N-(2-dimethylphosphorylphenyl)pyrimidine-2,4-diamine CAS 1197958-12-5

Synonyms:

AP26113;(2-((5-Chloro-2-((4-(4-(dimethylamino)piperidin-1-yl)-2-methoxyphen-yl)amino)pyrimidin-4-yl)ami;

Chemical & Physical Properties

Form:solid

Density:1.3±0.1 g/cm³

Boiling Point:737.6±70.0℃at 760 mmHg

Molecular Formula:C26H34ClN6O2P

Molecular Weight:529.014

Flash Point:399.9±35.7℃

Exact Mass:528.216919

PSA :95.66000

LogP:1.10

Vapour Pressure:0.0±2.4 mmHg at 25℃

Index of Refraction :1.626

Uses :

AP26113 is an effective ALK inhibitor with an IC50 of 0.62 nM, which can overcome the resistance of Crisotinib mediated by L1196M mutation.

AP26113 is highly effective in both sensitive and drug-resistant H3122 cells, reducing cell growth, inhibiting ALK phosphate, and inducing cell apoptosis in a dose-dependent manner. AP26113 acts on H3122 and H3122CR cells, reducing p-ALK with 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 IC50 of 10 nM and 24 nM, respectively. AP26113 inhibits the growth of SU-DHL-1, H3122, and Ba/F3-EML4-ALKv1 cell lines, with GI50 values of 9nM, 4nM, and 13nM, respectively. AP26113 acts on Karpas-299, SU-DHL-1, and L-82 cell lines, inhibiting ALK phosphorylation with IC50 of 3.2 nM, 1.5 nM, and 2.1 nM, respectively. AP26113 acts on Karpas-299 and H3122 cells, inhibiting ALK and ERK phosphorylation in a dose-dependent manner. AP26113 acts on Ba/F3 cell line (including wild type EML4-ALK) and Ba/F3 cell line (including Mutant EML4-ALKG1269S) to inhibit cell growth, with IC50 of 11nM and 16nM respectively. AP26113 acts on Ba/F3 cell line (including wild type EML4-ALK) and Ba/F3 cell line (including Mutant EML4-ALKE1210ChemicalbookK) to inhibit cell growth and ALK phosphorylation, with IC50 of 74 nM and 335 nM respectively. AP26113 (10mg/kg-75mg/kg) is highly effective in anti PF-02341066 EML4-ALK Mutant mouse tumor transplantation model. AP26113 acts on tumors expressing wild type EML4-ALK, G1269S and L1196M Mutant at 25 mg/kg, 50 mg/kg and 50 mg/kg doses to induce tumor regression. AP26113 acts on Ba/F3 cells expressing EGFR-DEL, inhibiting EGFR phosphorylation and activity, with IC50 of 75 nM and 114 nM, respectively. AP26113 acts on Ba/F3 cells expressing EGFR DEL/T790M, inhibiting EGFR phosphorylation and activity, with IC50 of 15 and 281nM, respectively. AP26113 acts on NSCLC cell lines expressing EGFR DEL (HCC827), inhibiting EGFR phosphorylation with an IC50 of 62 nM and also inhibiting cell growth with a GI50 of 165 nM. AP26113 acts on HCC827 cell lines expressing EGFR DEL/T790M, inhibiting EGFR phosphorylation with an IC50 of 59nM and also inhibiting cell growth with a GI50 of 245nM.AP26113 acts on HCC78 NSCLC cells, effectively inhibiting SLC34A2-ROS driven signaling and proliferation, and this effect is dose-dependent.

If you are interested in our products or have any questions, please feel free to contact us!

Products under patent are offered for R & D purpose only. However, the final responsibility lies exclusively with the buyer.