Dalmelitinib
Based on 1 Customer Validation
Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.65%
- CAS No.: 1637658-98-0
- Formule: C22H16FN7O2S
- Masse moléculaire:461.47
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Kinase Inhibitor Library
HY-L009
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Protein Tyrosine Kinase Compound Library
HY-L016
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Posttranslational Modification Library
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>10000 nM
Compound: 4d
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Cytotoxicity against human A549 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
Cytotoxicity against human A549 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
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[PMID: 27288183] |
| HCCLM3 | IC50 |
33 nM
Compound: 4d
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Cytotoxicity against human HCCLM3 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
Cytotoxicity against human HCCLM3 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
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[PMID: 27288183] |
| Huh-7 | IC50 |
>10000 nM
Compound: 4d
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Cytotoxicity against human HuH7 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
Cytotoxicity against human HuH7 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
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[PMID: 27288183] |
| MHCC97H | IC50 |
6 nM
Compound: 4d
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Cytotoxicity against human MHCC97H cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
Cytotoxicity against human MHCC97H cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
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[PMID: 27288183] |
| MKN-45 | IC50 |
6 nM
Compound: 4d
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Cytotoxicity against human MKN45 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
Cytotoxicity against human MKN45 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
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[PMID: 27288183] |
| NCI-H1975 | IC50 |
>10000 nM
Compound: 4d
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Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
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[PMID: 27288183] |
| NCI-H1993 | IC50 |
14 nM
Compound: 4d
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Cytotoxicity against human NCI-H1993 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
Cytotoxicity against human NCI-H1993 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
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[PMID: 27288183] |
| NCI-N87 | IC50 |
>10000 nM
Compound: 4d
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Cytotoxicity against human NCI-N87 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
Cytotoxicity against human NCI-N87 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
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[PMID: 27288183] |
| SNU-5 | IC50 |
2 nM
Compound: 4d
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Cytotoxicity against human SNU5 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
Cytotoxicity against human SNU5 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
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[PMID: 27288183] |
Dalmelitinib (Compound 4 d) binds to the ATP-binding region of c-Met kinase, and shows slective inhibitory activity against c-Met with an IC50 value of 2.9 nM[1].
Dalmelitinib (0-1 μM approximately, 3 days) inhibits cell proliferation in various c-Met oncogene amplification cancer cell lines, with IC50 values ranging from 6 nM to 33 nM[1].
Dalmelitinib (0.1-1 μM, 6-24 h) significantly induces the phosphorylation of the tyrosine kinases (MET), partially or completely inhibits the downstream phosphorylation of ERK and AKT in HCCLM3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C-Met oncogene amplification cancer cell: SNU-5, HCCLM3, MHCC97-H, MHCC97-L, MKN-45, NCI-H1993.
No C-Met oncogene amplification cancer cell: Huh-7, NCI-N87, NCI-1975, A549. -
Concentration:0-1 μM approximately.
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Incubation Time:3 days
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Result:IC50: 33 nM (HCCLM3), 6 nM (MHCC97-H, MKN-45), 7 nM (MHCC97-L), 14 nM (NCI-H1993), 2 nM (SNU-5); Other cells: > 1000 nM.
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Cell Line:C-Met oncogene amplification cancer cell: SNU-5, HCCLM3, MHCC97-H, MHCC97-L, MKN-45, NCI-H1993.
No C-Met oncogene amplification cancer cell: Huh-7, NCI-N87, NCI-1975, A549. -
Concentration:0.1, 0.3, 1 μM
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Incubation Time:6-24 h
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Result:Significantly induced the phosphorylation of the tyrosine kinases (MET), partially inhibited the downstream phosphorylation of AKT, and completely inhibited the downstream phosphorylation of ERK.
Dalmelitinib (intragastric administration, 5 mg/kg for a single dose) shows a high plasma concentration, longer half-life and mean residence time, low clearance rates in BALB/c small nude mice[1].
Dalmelitinib shows a high level of No Observed Adverse Effect Level (NOAEL) in mice long-term toxicity (225 mg/kg/day) and acute toxicity (600 mg/kg/day)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MKN-45 tumor xenograft nude mice[1]
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Dosage:10, 30, 60 mg/kg
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Administration:Intragastric administration
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Result:Inhibited the tumor growth with the inhibitory rates of 29.5% (10 mg/kg), 34.2% (30 mg/kg), and 61.4% (60 mg/kg).
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Animal Model:BALB/c small nude mice (pharmacokinetic assay)[1]
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Dosage:5 mg/kg for a single dose
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Administration:Intragastric administration
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Result:Pharmacokinetic profile of Dalmelitinib (Compound 4 d)
Compound Cmax (ng/mL) AUC (ng/mL/h) t1/2 (h) MRT (h) CL/F (mL/min/kg) Vz/F Dalmelitinib 8628 122487 5.55 9.10 0.68 327
Chemical Information
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CAS No. 1637658-98-0
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Appearance Solid
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Masse moléculaire 461.47
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Formule C22H16FN7O2S
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Color White to off-white
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SMILES
O=C1N(C)C2=CN=C3C=CC(SC4=NN=C5C(F)=CC(C6=CN(C)N=C6)=CN45)=CC3=C2OC1
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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 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (216.70 mM; ultrasonic and warming and heat to 80°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (5.42 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1670 mL | 10.8349 mL | 21.6699 mL | 54.1747 mL |
| 5 mM | 0.4334 mL | 2.1670 mL | 4.3340 mL | 10.8349 mL | |
| 10 mM | 0.2167 mL | 1.0835 mL | 2.1670 mL | 5.4175 mL | |
| 15 mM | 0.1445 mL | 0.7223 mL | 1.4447 mL | 3.6116 mL | |
| 20 mM | 0.1083 mL | 0.5417 mL | 1.0835 mL | 2.7087 mL | |
| 25 mM | 0.0867 mL | 0.4334 mL | 0.8668 mL | 2.1670 mL | |
| 30 mM | 0.0722 mL | 0.3612 mL | 0.7223 mL | 1.8058 mL | |
| 40 mM | 0.0542 mL | 0.2709 mL | 0.5417 mL | 1.3544 mL | |
| 50 mM | 0.0433 mL | 0.2167 mL | 0.4334 mL | 1.0835 mL | |
| 60 mM | 0.0361 mL | 0.1806 mL | 0.3612 mL | 0.9029 mL | |
| 80 mM | 0.0271 mL | 0.1354 mL | 0.2709 mL | 0.6772 mL | |
| 100 mM | 0.0217 mL | 0.1083 mL | 0.2167 mL | 0.5417 mL |
Dalmelitinib Related Classifications
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