| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| ln Vitro |
MDA-MB-231 tumor cells' motility is inhibited by NP-G2-044, with an IC50 of less than 10 μM. Filopodia development is decreased by NP-G2-044, which also decreases lamellipodia production [1].
|
|---|---|
| ln Vivo |
In mouse models, NP-G2-044 (100 mg/kg; intraperitoneally; once daily for 18 days) prevents the spread of breast tumors [1]. NP-G2-044 binds to myofacundum after terminating at the lateral wall, blocking the development of actin bundles and filopodia α. Tumor cell movement and appropriate cell morphology are facilitated by blocking actin cell remodeling.
|
| Animal Protocol |
Animal/Disease Models: 6-8 weeks old female BALB/c mouse (mouse model bearing 4T1 tumor cells) [1]
Doses: 100mg/kg Mode of Route of Administration: Ip; dynamic changes are damaged, and tumor cell migration and metastasis are inhibited [3]. one time/day for 18 days. Experimental Results: Inhibited the metastasis of 4T1 mouse mammary tumor cells to the lungs. |
| References | |
| Additional Infomation |
NP-G2-044 is currently undergoing clinical trials (NCT03199586) (Phase I clinical trial of the metastasis inhibitor NP-G2-044 for the treatment of patients with advanced or metastatic solid tumors (including lymphoma)). The Fascin inhibitor NP-G2-044 is an orally effective fascin protein inhibitor with potential antitumor activity. After oral administration, NP-G2-044 targets and binds to fascin, thereby preventing the interaction between fascin and actin filaments, and consequently inhibiting the formation of actin bundles and filopodia. By preventing the reorganization of the actin cytoskeleton, the morphological dynamics required for tumor cell migration and invasion are suppressed, thereby inhibiting tumor cell migration and metastasis. Fibronectin (fascin), the major actin crosslinking protein in filopodia, is upregulated in various metastatic tumor cells, but low or absent in normal adult epithelial cells; its expression is associated with aggressive phenotype, poor prognosis, and shortened survival. Filamentous pseudopodia are finger-like plasma membrane protrusions formed after actin cytoskeleton remodeling. They appear frequently in metastatic tumor cells, and their presence is associated with the invasiveness of tumor cells.
|
| Molecular Formula |
C21H16F3N3O2
|
|---|---|
| Molecular Weight |
399.3732
|
| Exact Mass |
399.119
|
| CAS # |
1807454-59-6
|
| PubChem CID |
91844684
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.36±0.1 g/cm3(Predicted)
|
| Boiling Point |
470.5±45.0 °C(Predicted)
|
| LogP |
4.7
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
29
|
| Complexity |
580
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
XLLRLAABUFOJPC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H16F3N3O2/c1-13-16(10-11-29-13)20(28)25-19-17-4-2-3-5-18(17)27(26-19)12-14-6-8-15(9-7-14)21(22,23)24/h2-11H,12H2,1H3,(H,25,26,28)
|
| Chemical Name |
2-methyl-N-[1-[[4-(trifluoromethyl)phenyl]methyl]indazol-3-yl]furan-3-carboxamide
|
| Synonyms |
NPG2-044; NP G2-044; NP-G2-044
|
| 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) |
DMSO : ~100 mg/mL (~250.39 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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 (6.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5039 mL | 12.5197 mL | 25.0394 mL | |
| 5 mM | 0.5008 mL | 2.5039 mL | 5.0079 mL | |
| 10 mM | 0.2504 mL | 1.2520 mL | 2.5039 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
