CH7057288 |
Catalog No.GC33112
One-Click Copy Product Info
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CH7057288 is a novel, orally active TRK inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2095616-82-1
Sample solution is provided at 25 µL, 10mM.
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CH7057288 is a novel, orally active TRK inhibitor. CH7057288 inhibits the activity of TRKA (IC50=1.1nM), TRKB (IC50=7.8nM), and TRKC (IC50=5.1nM) to block tumor cell proliferation, while also reducing tumor growth by inhibiting the MAPK and E2F signaling pathways. CH7057288 is suitable for research related to TRK fusion-positive cancers[1-2].
In vitro, treatment of TRK fusion-positive cell lines (such as NIH3T3 MPRIP-NTRK1 and CUTO-3) with CH7057288 (8.4–67nM) for 4–7 days. CH7057288 significantly inhibited cell proliferation[1]. CH7057288 (0.1µM-1mM) also inhibited the proliferation of TRK fusion-positive cell lines (including CUTO-3, KM12-Luc, and MO-91) after 4 or 7 days of treatment, by inhibiting TRK autophosphorylation to block MAPK and E2F signaling pathways[2].
In vivo, oral administration of CH7057288 (0.6-10mg/kg) once daily for 4 weeks to NCG mouse models bearing implanted TRK fusion-positive tumors (such as KM12-Luc). CH7057288 significantly inhibited tumor growth[2].
References:
[1] Ito T, Kinoshita K, Tomizawa M, et al. Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor. J Med Chem. 2022 Sep 22;65(18):12427-12444.
[2] Tanaka H, Sase H, Tsukaguchi T, et al. Selective TRK Inhibitor CH7057288 against TRK Fusion-Driven Cancer. Mol Cancer Ther. 2018 Dec;17(12):2519-2529.
| Cell experiment [1]: | |
Cell lines | TRK fusion-positive cancer cell lines (e.g., NIH3T3 MPRIP-NTRK1, CUTO-3, KM12-Luc) |
Preparation Method | TRK fusion-positive cancer cells were treated with CH7057288 (8.4–67nM) for 4 to 7 days. |
Reaction Conditions | 8.4–67nM; 4-7 days. |
Applications | CH7057288 potently inhibited the proliferation of TRK fusion-positive cell lines by inhibiting TRK auto-phosphorylation and blocking downstream MAPK and E2F signaling pathways. |
| Animal experiment [2]: | |
Animal models | NCG mice bearing subcutaneous NIH3T3 MPRIP-NTRK1 tumors (or CUTO-3 NSCLC xenografts) |
Preparation Method | Mice were orally administered CH7057288 (0.6-10mg/kg) once daily for 4 weeks. |
Dosage form | 0.6-10mg/kg; p.o.; Daily for 4 weeks. |
Applications | CH7057288 induced potent tumor growth inhibition in the NIH3T3 MPRIP-NTRK1 model and CUTO-3 model. Importantly, no significant body weight loss was observed. |
References: | |
| Cas No. | 2095616-82-1 | SDF | |
| Canonical SMILES | O=C1C2=C(OC3=CC(C#CC4=CC(C(NC(C)(C)C)=O)=CC(C)=N4)=CC=C23)C(C)(C)C5=CC(NS(C)(=O)=O)=CC=C15 | ||
| Formula | C32H31N3O5S | M.Wt | 569.67 |
| Solubility | DMSO : ≥ 34 mg/mL (59.68 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7554 mL | 8.777 mL | 17.554 mL |
| 5 mM | 351.1 μL | 1.7554 mL | 3.5108 mL |
| 10 mM | 175.5 μL | 877.7 μL | 1.7554 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)