| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| ln Vitro |
Dalmelitinib (compound 4 d) binds to the ATP-binding domain of c-Met kinase and exhibits 2.9 nM IC50 selective inhibitory action against c-Met [1]. With IC50 values ranging from 6 nM to 33 nM, damelitinib (about 0-1 μM, 3 days) reduces cell proliferation in a variety of c-Met oncogene-amplified cancer cell lines [1]. In HCCLM3 cells, damelitinib (0.1–1 μM, 6–24 h) strongly increases tyrosine kinase (MET) phosphorylation and either totally or partially suppresses ERK and AKT phosphorylation downstream [1].
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| ln Vivo |
Dalmelitinib (compound 4 d, intragastric injection, 10-60 mg/kg) effectively suppressed tumor growth in MKN-45 tumor xenograft nude mice in a dose-dependent manner [1]. Damatinib (given by gavage, single dose 5 mg/kg) showed high blood concentration, extended half-life and mean residence time, and low clearance rate in BALB/c nude mice [1]. Dalmelitinib revealed significant no-observed adverse effect levels (NOAELs) in long-term toxicity (225 mg/kg/day) and acute toxicity (600 mg/kg/day) in mice [1].
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| Cell Assay |
Cell proliferation experiment [1]
Cell Types: C-Met oncogene amplified cancer cells: SNU-5, HCCLM3, MHCC97-H, MHCC97-L, MKN-45, NCI-H1993. Cancer cells without C-Met oncogene amplification: Huh-7, NCI-N87, NCI-1975, A549. Tested Concentrations: approximately 0-1μM. Incubation Duration: 3 days Experimental Results: 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. Western Blot Analysis [1] Cell Types: C-Met oncogene amplified cancer cells: SNU-5, HCCLM3, MHCC97-H, MHCC97-L, MKN-45, NCI-H1993. Cancer cells without C-Met oncogene amplification: Huh-7, NCI-N87, NCI-1975, A549. Tested Concentrations: 0.1, 0.3, 1 μM Incubation Duration: 6-24 h Experimental Results: Dramatically induced tyrosine kinase (MET) phosphorylation, partially inhibited AKT downstream phosphorylation, and completely inhibited ERK downstream phosphorylation. |
| Animal Protocol |
Animal/Disease Models: MKN-45 tumor xenograft nude mice [1]
Doses: 10, 30, 60 mg/kg Route of Administration: intragastric (po) (po)administration Experimental Results: Inhibited tumor growth, the inhibition rates were 29.5% (10 mg/kg), 34.2 % (10 mg/kg). 30 mg/kg) and 61.4% (60 mg/kg). Animal/Disease Models: BALB/c nude mice (pharmacokinetic/PK/PK determination) [1] Doses: single dose 5 mg/kg Route of Administration: intragastric (po) (po)administration Experimental Results: pharmacokinetic/PK/PK characteristics of dametinib (compound 4d) Compound Cmax (ng/mL) AUC (ng/mL/h) t1/2 (h) MRT (h) CL/F (mL/min/kg) Vz/F Damitinib 8628 122487 5.55 9.10 0.68 327 |
| References |
| Molecular Formula |
C22H16FN7O2S
|
|---|---|
| Molecular Weight |
461.471545219421
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| Exact Mass |
461.107
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| CAS # |
1637658-98-0
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| PubChem CID |
86302574
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| Appearance |
White to off-white solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
33
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| Complexity |
752
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1C2C(=CC(SC3N4C(=NN=3)C(F)=CC(C3=CN(C)N=C3)=C4)=CC=2)C2OCC(=O)N(C)C=2C=1
|
| InChi Key |
MFEXYTURXUZOID-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H16FN7O2S/c1-28-9-13(7-25-28)12-5-16(23)21-26-27-22(30(21)10-12)33-14-3-4-17-15(6-14)20-18(8-24-17)29(2)19(31)11-32-20/h3-10H,11H2,1-2H3
|
| Chemical Name |
9-[[8-fluoro-6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl]sulfanyl]-4-methyl-[1,4]oxazino[3,2-c]quinolin-3-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~216.7 mM; with ultrasonication and warming by heating to 80°C)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.42 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.42 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1670 mL | 10.8349 mL | 21.6699 mL | |
| 5 mM | 0.4334 mL | 2.1670 mL | 4.3340 mL | |
| 10 mM | 0.2167 mL | 1.0835 mL | 2.1670 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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