| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Glesatinib (MGCD-265) is an orally bioavailable and multitargeted tyrosine kinase (MET/SMO) inhibitor with potential anticancer activity. It antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
| ln Vitro |
Glesatinib (MGCD265; 0.01-5 μM; for 72 hours) inhibits the proliferation of cancer cells in a dose-dependent manner and has a low IC50 value of 0.08 μM on NSCLC H1299 cells[1]. The percentage of apoptotic cells in NSCLC H1299 cells is dramatically increased by several times when glesatinib (0.01, 0.1, 0.5, and 1 μM) is added[1]. KB-C2, SW620/Ad300, HEK293/ABCB1, and their parent cells KB-3-1, SW620, and HEK293 cells exhibit cytotoxicity towards P-gp overexpressing cancer cells when exposed to glesatinib, with IC50 values ranging from 5 to 10 μM[1]. Within 120 minutes, glesatinib (1, 3 μM) raises the intracellular [3H]-Paclitaxel build-up and suppression [3H]-Paclitaxel efflux in P-gp-overexpressing cancer cell lines[2]. P-gp transporters' ATPase activity is dose-dependently stimulated by glesatinib (0–40 μM)[2].
|
|---|---|
| ln Vivo |
The drug glesatinib (MGCD265; oral; 15 mg/kg/day; 40 weeks) significantly reduces tumor size[1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: NSCLC H1299 cells Tested Concentrations: 0.01, 0.1, 1, 2, 5 μM Incubation Duration: For 72 hrs (hours) Experimental Results: Resulted in a dose-dependent inhibition of cancer cell growth and demonstrated the lowest IC50 value of 0.08 μM. |
| Animal Protocol |
Animal/Disease Models: 4−6-week old female balb/c athymic (nu/nu) mice with HCC827 NSCLC tumor xenografts[1]
Doses: 15 mg/kg Route of Administration: po (oral gavage) daily; 40 weeks Experimental Results: Caused a significant decrease in tumor size. |
| References |
|
| Additional Infomation |
Glesatinib is an orally bioavailable, small-molecule, multitargeted tyrosine kinase inhibitor with potential antineoplastic activity. Glesatinib binds to and inhibits the phosphorylation of several receptor tyrosine kinases (RTKs), including the c-Met receptor (hepatocyte growth factor receptor); the Tek/Tie-2 receptor; vascular endothelial growth factor receptor (VEGFR) types 1, 2, and 3; and the macrophage-stimulating 1 receptor (MST1R or RON). Inhibition of these RTKs and their downstream signaling pathways may result in the inhibition of tumor angiogenesis and tumor cell proliferation in tumors overexpressing these RTKs.
Drug Indication Investigated for use/treatment in cancer/tumors (unspecified). |
| Molecular Formula |
C31H27F2N5O3S2
|
|---|---|
| Molecular Weight |
619.7058
|
| Exact Mass |
619.152
|
| CAS # |
936694-12-1
|
| Related CAS # |
Glesatinib hydrochloride;1123838-51-6
|
| PubChem CID |
25181472
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.4±0.1 g/cm3
|
| Index of Refraction |
1.672
|
| LogP |
6.5
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
43
|
| Complexity |
902
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S1C2C(=CC=NC=2C=C1C1C=CC(=CN=1)CNCCOC)OC1C=CC(=CC=1F)NC(NC(CC1C=CC(=CC=1)F)=O)=S
|
| InChi Key |
YRCHYHRCBXNYNU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C31H27F2N5O3S2/c1-40-13-12-34-17-20-4-8-24(36-18-20)28-16-25-30(43-28)27(10-11-35-25)41-26-9-7-22(15-23(26)33)37-31(42)38-29(39)14-19-2-5-21(32)6-3-19/h2-11,15-16,18,34H,12-14,17H2,1H3,(H2,37,38,39,42)
|
| Chemical Name |
N-[[3-fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]pyridin-2-yl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]carbamothioyl]-2-(4-fluorophenyl)acetamide
|
| Synonyms |
MGCD265 MGCD 265 MGCD-265
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6137 mL | 8.0683 mL | 16.1366 mL | |
| 5 mM | 0.3227 mL | 1.6137 mL | 3.2273 mL | |
| 10 mM | 0.1614 mL | 0.8068 mL | 1.6137 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
