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ALK-IN-1
🥰Excellent
Catalog No. T3059Cas No. 1197958-12-5
Alias Brigatinib-analog, AP26113-analog, AP26113
ALK-IN-1 (AP26113) is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2.
ALK-IN-1
🥰Excellent
Purity: 100%
Catalog No. T3059Alias Brigatinib-analog, AP26113-analog, AP26113Cas No. 1197958-12-5
ALK-IN-1 (AP26113) is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $40 | In Stock | |
| 10 mg | $64 | In Stock | |
| 25 mg | $97 | In Stock | |
| 50 mg | $147 | In Stock | |
| 100 mg | $247 | In Stock | |
| 200 mg | $367 | In Stock | |
| 500 mg | $595 | In Stock |
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Purity:100%
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.Product Introduction
Bioactivity
Chemical Properties
| Description | ALK-IN-1 (AP26113) is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2. |
| Targets&IC50 | ALK:0.62 nM |
| In vitro | In HCC827 (EGFR-DEL) or HCC827 (EGFR-DEL/T790M) transplantation tumor mouse models, AP26113 (25 mg/kg), inhibited tumor cell growth. In the Karpas-299 transplantation tumor mouse model, AP26113 (<50 mg/kg) inhibited p-ALK. In the Karpas-299 transplantation tumor mouse model and the H3122 transplantation tumor mouse model, AP26113 (<50 mg/kg) inhibited tumor growth. |
| In vivo | Leflunomide inhibited growth in SU-DHL-1 (GI50=9 nM), H3122 (GI50=4 nM) and Ba/F3-EML4-ALK v1 (1 gI50=3 nM) cell lines. In NSCLC cell lines expressing EGFR-DEL (HCC827) (IC50=62 nM), AP26113 acted to inhibit EGFR phosphorylation and inhibited cell growth. |
| Cell Research | Three-day cell viability assays are carried out by plating 2,000, 1,500 and 2,000 cells per well of Ba/F3, PC9 or MGH121, respectively, into black transparent-bottom 96-well plates. On the same day for Ba/F3 cells and the following day for PC9 and MGH121 cells, the cells are treated with each TKI across a 10-dose range from 0.3 nM to 10 μM. After 72 h of drug treatment, cell viability is measured using the CellTiter-Glo assay. (Only for Reference) |
| Alias | Brigatinib-analog, AP26113-analog, AP26113 |
| Molecular Weight | 529.01 |
| Formula | C26H34ClN6O2P |
| Cas No. | 1197958-12-5 |
| Smiles | N(C1=C(P(C)(C)=O)C=CC=C1)C2=NC(NC3=C(OC)C=C(C=C3)N4CCC(N(C)C)CC4)=NC=C2Cl |
| Relative Density. | 1.29 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 98 mg/mL (185.3 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 1 mg/mL, Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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