AP26113-ANALOG
Brigatinib-analog
CAS: 1197958-12-5
Molecular Formula: C26H34ClN6O2P
AP26113-ANALOG - Names and Identifiers
AP26113-ANALOG - Physico-chemical Properties
| Molecular Formula | C26H34ClN6O2P |
| Molar Mass | 529.01 |
| Density | 1.29±0.1 g/cm3(Predicted) |
| Boling Point | 737.6±70.0 °C(Predicted) |
| pKa | 9.27±0.20(Predicted) |
| Storage Condition | -20℃ |
AP26113-ANALOG - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.89 ml | 9.452 ml | 18.903 ml |
| 5 mM | 0.378 ml | 1.89 ml | 3.781 ml |
| 10 mM | 0.189 ml | 0.945 ml | 1.89 ml |
| 5 mM | 0.038 ml | 0.189 ml | 0.378 ml |
Last Update：2024-01-02 23:10:35
AP26113-ANALOG - Uses and synthesis methods
biological activity
AP26113 is an effective ALK inhibitor with IC50 of 0.62 nM, which can overcome the Crizotinib resistance mediated by L1196M mutation. Phase 2.
in vitro studies
AP26113 is highly effective in sensitive and drug-resistant H3122 cells, reducing cell growth, inhibiting ALK phosphate, and inducing apoptosis. This effect is dose-dependent. AP26113 acts on H3122 and H3122 CR cells to reduce p-ALK,IC50 is 7.4 and 16.8 nM respectively. AP26113 acts on Ba/F3 cells expressing wild-type or mutant EML4-ALK to reduce the number of cells with IC50 of 10 nM and 24 nM respectively. AP26113 inhibited the growth of SU-DHL-1, H3122 and Ba/F3-EML4-ALK v1 cell lines with GI50 of 9 nM, 4 nM and 13 nM, respectively. AP26113 acts on Karpas-299, SU-DHL-1 and L-82 cell lines to inhibit ALK phosphorylation with IC50 of 3.2 nM, 1.5 nM and 2.1 nM respectively. AP26113 acts on Karpas-299 and H3122 cells to inhibit ALK and ERK phosphorylation, which is dose-dependent. AP26113 acts on Ba/F3 cell line (including wild-type EML4-ALK) and Ba/F3 cell line (including mutant EML4-ALK G1269S) to inhibit cell growth with 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 (including mutant EML4-ALK E1210K) to inhibit cell growth and ALK phosphorylation with IC50 of 74 nM and 335 nM respectively. AP26113(10 mg/kg-75 mg/kg) effectively acted on anti-PF-02341066 EML4-ALK mutant mouse transplanted tumor model. AP26113 25 mg/kg, 50 mg/kg and 50 mg/kg doses were applied to tumors expressing wild-type EML4-ALK, G1269S and L1196M mutant types to induce tumor decline. AP26113 acts on EGFR-DEL-expressing Ba/F3 cells and inhibits EGFR phosphorylation and activity. IC50 is 75 nM and 114 nM respectively. AP26113 acts on Ba/F3 cells expressing EGFR-DEL/T790M to inhibit EGFR phosphorylation and activity with IC50 of 15 and 281 nM respectively. AP26113 acts on NSCLC cell line expressing EGFR-DEL(HCC827) to inhibit EGFR phosphorylation, IC50 is 62nM, and cell growth is also inhibited, GI50 is 165 nM. AP26113 acts on HCC827 cell line expressing EGFR-DEL/T790M, inhibits EGFR phosphorylation, IC50 is 59 nM, and also inhibits cell growth, GI50 is 245 nM. AP26113 acts on HCC78 NSCLC cells to effectively inhibit SLC34A2-ROS-driven signals and proliferation in a dose-dependent manner.
In vivo studies
AP26113(<50 mg/kg) acts on Karpas-299 transplanted tumor mouse model and inhibits p-ALK. This effect is dose-dependent. AP26113(< 50 mg/kg) acts on Karpas-299 transplanted tumor mouse model and H3122 transplanted tumor mouse model to inhibit tumor growth in a dose-dependent manner. AP26113 have good performance, including moderate plasma protein binding in vitro (47%,70% and 76% acting on human, rat and mouse respectively), and have little inhibitory effect on the main CYP subtypes. Rats treated with AP26113 (10 mg/kg) were well tolerated with Cmax of 2587 ng/mL and AUC of 41120 hr.ng/mL. AP26113 (25 mg/kg) acts on HCC827(EGFR-DEL) or HCC827(EGFR-DEL/T790M) transplanted tumor mouse models, resulting in tumor decline.
features
AP26113 inhibition of ALK is at least 10 times more effective and selective than Crizotinib.
Last Update：2024-04-09 01:59:50
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Spot supply
Product Name: Brigatinib Impurity 5 Visit Supplier Webpage Request for quotationCAS: 1197958-12-5
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: AP26113 Visit Supplier Webpage Request for quotationCAS: 1197958-12-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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