| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Bax
|
|---|---|
| ln Vitro |
For MDA-MB-231 and MCF-7 breast cancer cell lines, GL0388 (0.1–10 μM; 72 h) suppresses cell growth with IC50s of 0.96 μM and 0.52 μM, respectively[1]. With GI550s of 0.299-1.57 μM, GL0388 (0.01-100 μM) suppresses the growth of 60 human tumor cell lines[1]. In MDA-MB-231 cells, GL0388 (1-10 μM; 48 h) dramatically increases the levels of cleaved PARP-1 and cleaved caspase 3 [1]. Breast cancer cell invasion and colony formation are inhibited by GL0388 (0.1–1 μM; 24 h)[1]. In a dose-dependent manner, GL0388 (1-10 μM; 24 h) facilitates Bax insertion into the mitochondrial membranes of MDA-MB-231 cells. In the cytosolic fraction of MDA-MB-231 cells, GL0388 raises cytochrome c[1].
|
| ln Vivo |
The growth of MDA-MB-231 tumors in mice is dose-dependently suppressed by GL0388 (10–20 mg/kg for ip; 15 mg/kg for it); administered once daily for 10 days[1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MCF-7, MDA-MB-231 cells Tested Concentrations: 0.1, 0.33, 1, 3.3, 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited the growth of MCF-7, MDA-MB-231 cells, with IC50s of 0.52 μM and 0.96 μM, respectively. Western Blot Analysis[1] Cell Types: MDA-MB-231 cells Tested Concentrations: 1, 5, 10 μM Incubation Duration: 48 hrs (hours) Experimental Results: Dramatically led to the upregulation of cleaved PARP -1 and cleaved caspase 3. |
| Animal Protocol |
Animal/Disease Models: Female nude mice were injected MDA-MB-231 cells[1]
Doses: 10-20 mg/kg for ip; 15 mg/kg for it Route of Administration: Ip and it one time/day for 10 days Experimental Results: Dramatically inhibited tumor growth at a dose of 15 mg/kg every other day. IT administration for 10 days, with an inhibition rate of 55%, comparable to the IP efficacy at the dose of daily 20 mg/ kg. |
| References |
| Molecular Formula |
C21H17FN2O
|
|---|---|
| Molecular Weight |
332.370888471603
|
| Exact Mass |
332.132
|
| CAS # |
2886772-68-3
|
| PubChem CID |
162640853
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
3.5
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
25
|
| Complexity |
483
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC=C\2C(=C1)C3=C(/C2=C/C4=C(N=CC=C4)OCCN)C=C(C=C3)F
|
| InChi Key |
WCVGRSPKTHQNCR-XDHOZWIPSA-N
|
| InChi Code |
InChI=1S/C21H17FN2O/c22-15-7-8-18-16-5-1-2-6-17(16)19(20(18)13-15)12-14-4-3-10-24-21(14)25-11-9-23/h1-8,10,12-13H,9,11,23H2/b19-12+
|
| Chemical Name |
2-[3-[(E)-(2-fluorofluoren-9-ylidene)methyl]pyridin-2-yl]oxyethanamine
|
| 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 (~300.9 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.52 mM) (saturation unknown) 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.
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 (7.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (7.52 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 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 | 3.0087 mL | 15.0435 mL | 30.0870 mL | |
| 5 mM | 0.6017 mL | 3.0087 mL | 6.0174 mL | |
| 10 mM | 0.3009 mL | 1.5043 mL | 3.0087 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
