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APS03118
Catalog No. T213623 Copy Product Info
🥰Excellent
APS03118 is an orally effective, potent, and highly selective RET inhibitor. It broadly inhibits RET fusions and various mutations (including G810, V804, L730, and Y806 variants), with IC50 values generally below 1 nM (0.0952 nM for the wild type; mutation IC50s range from 0.00438 to 5.72 nM), demonstrating significant inhibitory activity against RETG810 mutations. APS03118 effectively suppresses the entire RET signaling pathway, including RET, Shc, and ERK1/2, and shows more than 20-fold selectivity over most off-target kinases, excluding FLT3 and YES. In vivo, APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804M PDX mouse models and significantly extends survival in intracranial CCDC6-RET metastatic mouse models. This compound is applicable for research on RET-driven cancers resistant to selective RET inhibitors (SRI).
APS03118
Copy Product Info🥰Excellent
Catalog No. T213623
APS03118 is an orally effective, potent, and highly selective RET inhibitor. It broadly inhibits RET fusions and various mutations (including G810, V804, L730, and Y806 variants), with IC50 values generally below 1 nM (0.0952 nM for the wild type; mutation IC50s range from 0.00438 to 5.72 nM), demonstrating significant inhibitory activity against RETG810 mutations. APS03118 effectively suppresses the entire RET signaling pathway, including RET, Shc, and ERK1/2, and shows more than 20-fold selectivity over most off-target kinases, excluding FLT3 and YES. In vivo, APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804M PDX mouse models and significantly extends survival in intracranial CCDC6-RET metastatic mouse models. This compound is applicable for research on RET-driven cancers resistant to selective RET inhibitors (SRI).
APS03118
Cas No. 2598870-24-5
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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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.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
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Chemical Properties
Storage & Solubility Information
| Description | APS03118 is an orally effective, potent, and highly selective RET inhibitor. It broadly inhibits RET fusions and various mutations (including G810, V804, L730, and Y806 variants), with IC50 values generally below 1 nM (0.0952 nM for the wild type; mutation IC50s range from 0.00438 to 5.72 nM), demonstrating significant inhibitory activity against RETG810 mutations. APS03118 effectively suppresses the entire RET signaling pathway, including RET, Shc, and ERK1/2, and shows more than 20-fold selectivity over most off-target kinases, excluding FLT3 and YES. In vivo, APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804M PDX mouse models and significantly extends survival in intracranial CCDC6-RET metastatic mouse models. This compound is applicable for research on RET-driven cancers resistant to selective RET inhibitors (SRI). |
| In vitro | APS03118 (compound 5) exhibits significantly greater inhibitory activity against RET solvent front G810 mutations compared to Selpercatinib and Pralsetinib. It also shows exceptional efficacy against RET resistant mutations, including solvent front and gatekeeper mutations, and demonstrates strong antiproliferative activity equivalent to that of Pralsetinib and Selpercatinib in natural RET fusion-positive LC2/ad lung cancer cells (IC 50 = 10.08 nM). APS03118 effectively inhibits RET autophosphorylation in Ba/F3 KIF5B-RET, Ba/F3 KIF5B-RET V804M, Ba/F3 KIF5B-RET G810R, and Ba/F3 KIF5B-RET M918T cells with IC 50 values of 1.91, 1.18, 14.66, and 2.28 nM, respectively. Furthermore, at low nanomolar concentrations (0-1000 nM, 1.5 hours), APS03118 effectively inhibits the entire RET signaling pathway, including RET, Shc, and ERK1/2, in TT-RET C634W cells. |
| In vivo | APS03118 administered at doses of 3, 10, and 30 mg/kg orally, twice daily for 28 consecutive days, demonstrates significant antitumor activity in KIF5B-RET and CCDC6-RET V804M PDX mouse models. Additionally, APS03118 given at 10 and 30 mg/kg, orally twice a day for 90 days, is effective in eliminating intracranial tumors and prolonging survival in mice with intracranial CCDC6-RET metastasis. Furthermore, APS03118 at doses of 10 and 30 mg/kg, administered orally twice daily for 14 or 15 days, inhibits tumor growth in Ba/F3 KIF5B-RET G810R and Ba/F3 KIF5B-RET V804M CDX mouse models. |
| Molecular Weight | 496.58 |
| Formula | C27H28N8O2 |
| Cas No. | 2598870-24-5 |
| Smiles | N=1N=C2NN3C=C(OCC)C=C(C=4C=NC(=CC4)N5CC6N(CC7=CN=C(OC)C=C7)C(C5)C6)C3=C2C1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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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 stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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