Elzovantinib
Based on 1 Customer Validation
Elzovantinib (TPX-0022) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 2271119-26-5
- Formula: C20H20FN7O2
- Molecular Weight:409.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 0.12 nM (SRC), 0.14 nM (MET), 0.76 nM (c-FMS)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MKN-45 | IC50 |
0.2 nM
Compound: 74
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Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell growth
Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell growth
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[PMID: 37262349] |
| SNU-5 | IC50 |
0.17 nM
Compound: 74
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Antiproliferative activity against human SNU-5 cells assessed as inhibition of cell growth
Antiproliferative activity against human SNU-5 cells assessed as inhibition of cell growth
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[PMID: 37262349] |
Elzovantinib (TPX-0022) causes the suppression of MET autophosphorylation as well as the downstream STAT3, ERK and AKT phosphorylation at IC50 values of around 1-3 nM in SNU-5 and MKN-45 cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Elzovantinib (p.o., BID, 10 days) demonstrates the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID and 15 mg/kg, BID, respectively in SCID/Beige mice[1].
Elzovantinib inhibits MET activity in MKN-45 tumors following oral administration in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice bearing LU2503 tumors patient derived xenograft (PDX) NSCLC model[1].
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Dosage:15 mg/kg.
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Administration:PO, BID (twice daily) for 13 days.
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Result:Resulted in an 85% tumor regression and no body weight loss was observed after 21 days treatment.
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Animal Model:SCID/Beige mice bearing Ba/F3 ETV6-CSF1R tumors with average tumor size of ~180 mm3[1].
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Dosage:5 and 15 mg/kg.
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Administration:PO, BID (twice daily) for 10 days.
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Result:Demonstrated the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID and 15 mg/kg, BID, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2271119-26-5
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Appearance Solid
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Molecular Weight 409.42
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Formula C20H20FN7O2
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Color White to off-white
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SMILES
N#CC1=C2CN(CC)C(C=C3)=NC(N3N=C4N)=C4C(NC[C@H](C)OC2=CC=C1F)=O
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Synonyms
TPX-0022; CSF1R-IN-2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 25 mg/mL (61.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. WO 2019023417 A1.
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4425 mL | 12.2124 mL | 24.4248 mL | 61.0620 mL |
| 5 mM | 0.4885 mL | 2.4425 mL | 4.8850 mL | 12.2124 mL | |
| 10 mM | 0.2442 mL | 1.2212 mL | 2.4425 mL | 6.1062 mL | |
| 15 mM | 0.1628 mL | 0.8142 mL | 1.6283 mL | 4.0708 mL | |
| 20 mM | 0.1221 mL | 0.6106 mL | 1.2212 mL | 3.0531 mL | |
| 25 mM | 0.0977 mL | 0.4885 mL | 0.9770 mL | 2.4425 mL | |
| 30 mM | 0.0814 mL | 0.4071 mL | 0.8142 mL | 2.0354 mL | |
| 40 mM | 0.0611 mL | 0.3053 mL | 0.6106 mL | 1.5265 mL | |
| 50 mM | 0.0488 mL | 0.2442 mL | 0.4885 mL | 1.2212 mL | |
| 60 mM | 0.0407 mL | 0.2035 mL | 0.4071 mL | 1.0177 mL |
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