Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
IC50: 2.9 nM (c‑Met)[1]
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ln Vitro |
D6808 exhibits 2.9 nM IC50 c-Met biochemical kinase inhibitory activity[1]. With an IC50 value of 0.7 nM, D6808 (0.0001-10 μM; 5 d) exhibits cellular antiproliferative efficacy against Hs746T cancer cells[1]. exhibits remarkable kinome selectivity, with IC50 values for Axl, TrkA, TrkB, and TrkC kinase, respectively, of 401.3, 437.2, 1386, and 203.9 nM[1]. With IC50 values of 4.3, 4.2, 3.2, 1.0, 39.0, and 33.4 nM for Ba/F3-Tpr-Met, Ba/F3-Tpr-MetF1200L, Ba/F3-Tpr-MetM1250T, Ba/F3 -Tpr-MetH1094Y, Ba/F3-Tpr-MetF1200I, and Ba/F3-Tpr-MetL1195V, respectively, D6808(0–10 μM; 72 h) exhibits antiproliferative potency to Tpr-Met fusion protein-transformed Ba/F3 cells[1]. In Ba/F3-Tpr-Met cells, D6808 (0-30 nM; 12 h) cleaves PARP and caspase-9 activation and dose-dependently reduces protein levels of CDK2, CDK4, CDK6, cyclin D2, and cyclin E1[1]. It also impacts MET activation. In Ba/F3-Tpr-Met cells, D6808 (40 nM; 24 h) causes 87.37% G0/G1 phase arrest and cell apoptosis[1].
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ln Vivo |
1.19 Rats' Pharmacokinetic Properties of D6808[1]. Fourth Rats Two milligrams per kilogram PO Rats 10.5 mg/kg IP Rats Tmax (h) 0.08 0.25 0.25 Cmax (ng/mL) 10.0 mg/kg T1/2 (h) 0.57 2.49 4.63 60.98 282.12 AUC0-T (h × ng/ml) 483.84 48.89 820.38 VZ (ML/KG) 3470.78 CL (ml/h/kg) 4207.06 MRT0-T (H) 0.71 3.40 F (%) 2.02 33.91
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: Hs746T cancer cell line Tested Concentrations: 0.0001-10 μM Incubation Duration: 5 days Experimental Results: Inhibited the cell proliferation of Hs746T cancer cells. Western Blot Analysis[1] Cell Types: Hs746T and Ba/F3-Tpr-Met cell lines Tested Concentrations: 0, 0.37, 1.1, 3.3, 10 and 30 nM Incubation Duration: 12 hrs (hours) Experimental Results: Suppressed the activation of MET in Hs746T and Ba/F3-Tpr-Met cells. Apoptosis Analysis[1] Cell Types: Ba/F3-Tpr-Met cell line Tested Concentrations: 40 nM Incubation Duration: 24 hrs (hours) Experimental Results: Induced 50.89% apoptosis after 48 h treatment. |
References |
[1]. Wang C, et al. Discovery of D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring MET Gene Alteration Treatment. J Med Chem. 2022 Nov 24;65(22):15140-15164.
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Molecular Formula |
C30H25F3N6O2
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Molecular Weight |
558.55
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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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7904 mL | 8.9518 mL | 17.9035 mL | |
5 mM | 0.3581 mL | 1.7904 mL | 3.5807 mL | |
10 mM | 0.1790 mL | 0.8952 mL | 1.7904 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.