Altiratinib
Based on 1 publication(s) in Google Scholar
Altiratinib (DCC-2701) is a multi-targeted kinase inhibitor with IC50s of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3, Trk1, Trk2, and Trk3 respectively.
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- Pureté: 99.29%
- CAS No.: 1345847-93-9
- Formule: C26H21F3N4O4
- Masse moléculaire:510.46
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Altiratinib
MoreVoir tous les produits spécifiques à Isoform VEGFR
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Activité biologique
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VEGFR2 9.2 nM (IC50) |
Trk1 0.85 nM (IC50) |
Trk2 4.6 nM (IC50) |
Trk3 0.93 nM (IC50) |
MET 2.7 nM (IC50) |
TIE2 8 nM (IC50) |
FLT3 9.3 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
0.00069 μM
Compound: 25; DCC2701
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Antiproliferative activity against human K562 cells
Antiproliferative activity against human K562 cells
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[PMID: 30188734] |
| K562 | IC50 |
0.69 nM
Compound: 25; DCC2701
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Antiproliferative activity against human K562 cells
Antiproliferative activity against human K562 cells
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[PMID: 30188734] |
| KM12 | IC50 |
0.0014 μM
Compound: 25; DCC2701
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Antiproliferative activity against human KM12 cells
Antiproliferative activity against human KM12 cells
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[PMID: 30188734] |
| SK-N-SH | IC50 |
0.0012 μM
Compound: 25; DCC2701
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Antiproliferative activity against human SK-N-SH cells
Antiproliferative activity against human SK-N-SH cells
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[PMID: 30188734] |
Altiratinib also inhibits MET isoforms METD1228H, MET D1228N, METY1230C, METY1230D, METY1230H, METM1250T with IC50s of 3.6, 1.3, 1.2, 0.37, 1.5 and 6 nM, respectively. Altiratinib inhibits MET phosphorylation with IC50 values of 0.85 and 2.2 nM, respectively. In the U-87 glioblastoma cell line, MET and HGF are both expressed. Altiratinib blocks autocrine activation of MET phosphorylation in these cells (IC50=6.2 nM). Altiratinib potently inhibits cellular proliferation in MET-amplified EBC-1 and MKN-45 cells, as well as TPM3-TRKA fusion KM-12 cells. Activation of MET is known to increase the motility and invasiveness of cancer cells: Altiratinib inhibits HGF-induced A549 cell migration, with an IC50 of 13 nM. Altiratinib also inhibits FLT3-ITD mutant MV-4-11 cell proliferation with an IC50 of 12 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1345847-93-9
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Appearance Solid
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Masse moléculaire 510.46
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Formule C26H21F3N4O4
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Color Light yellow to khaki
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SMILES
O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC(F)=C(OC4=CC(NC(C5CC5)=O)=NC=C4)C=C3F
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Synonyms
DCC-2701
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
DMSO : 25 mg/mL (48.98 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: ≥ 2.5 mg/mL (4.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocole
Altiratinib is dispensed into assay plates. Cells are added to 96-well (EBC-1, M-NFS-60, and SK-MEL-28: 2,500 cells/well; MKN-45: 5,000 cells/well; MV-4-11: 10,000 cells/well) or 384-well plates (A375 and HCT-116: 625 cells/well; BT-474, KM-12, PC-3, and U-87-MG: 1,250 cells/well). Plates are incubated for 72 hours. Viable cells are quantified using resazurin using a plate reader with excitation at 540 nm and emission at 600 nm[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Female nude mice are inoculated subcutaneously. On days 9 to 10, when tumor volumes reached 326 mg on average, mice are randomly assigned to groups and dosed once orally with 0.4% HMPC, (n=3); Altiratinib at 30 mg/kg (n=21); or Altiratinib at 10 mg/kg (n=21). At specified time points, whole blood and tumors are collected. Pharmacokinetic analysis is performed. Tumor samples are processed in the Western blot assay methods[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (566 KB)
- English - EN (566 KB)
- Français - FR (566 KB)
- Deutsch - DE (566 KB)
- Norwegian - NO (566 KB)
- Español - ES (566 KB)
- Swedish - SV (566 KB)
- Italian - IT (566 KB)
- Korean - KR (566 KB)
- Portuguese - PT (566 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 1.9590 mL | 9.7951 mL | 19.5902 mL | 48.9754 mL |
| 5 mM | 0.3918 mL | 1.9590 mL | 3.9180 mL | 9.7951 mL | |
| 10 mM | 0.1959 mL | 0.9795 mL | 1.9590 mL | 4.8975 mL | |
| 15 mM | 0.1306 mL | 0.6530 mL | 1.3060 mL | 3.2650 mL | |
| 20 mM | 0.0980 mL | 0.4898 mL | 0.9795 mL | 2.4488 mL | |
| 25 mM | 0.0784 mL | 0.3918 mL | 0.7836 mL | 1.9590 mL | |
| 30 mM | 0.0653 mL | 0.3265 mL | 0.6530 mL | 1.6325 mL | |
| 40 mM | 0.0490 mL | 0.2449 mL | 0.4898 mL | 1.2244 mL |
Altiratinib Related Classifications
HY-B0791 Related Classifications
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