| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| ln Vitro |
HuTel21 G4 and hTERT G4 have a quarterly affinity for SOP1812 (0 -800 nM; 6-24 h) [1]. 40 nM; 6–24 hours) impacts the pigments Rap1, Hippo, MAPK, and Wnt/β-catenin [1].
|
|---|---|
| ln Vivo |
MIA PaCa-2 xenograft mice and KPC transplanted mice demonstrated anti-tumor activity in response to intravenous administration of SOP1812 (1 mg/kg) once or twice weekly for 28 days [1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MIA PaCa-2, PANC-1, Capan- 1 and BxPC-3 Cell Line Tested Concentrations: 0-50 nM Incubation Duration: 96 hrs (hours) Experimental Results: For MIA PaCa-2, PANC-1, Capan-1 and BxPC-3 cells have anti-proliferative abilities, with GI50 values of 1.3, 1.4, 5.9 and 2.6 nM, respectively. Cell viability assay [1] Cell Types: PANC-1 Cell Tested Concentrations: 0, 100, 400 and 800 nM Incubation Duration: 6 and 24 hrs (hours) Experimental Results: Binding to hTERT G4 and HuTel21 G4, KD values were 4.9 and 28.4 nM respectively. Cell viability assay[1] Cell Types: MIA PaCa-2 Cell Tested Concentrations: 40 nM Incubation Duration: 6 hrs (hours) and 24 hrs (hours) Experimental Results: WNT5B, DVL1, AXIN and APC2 expression were affected, including the Wnt/β-catenin pathway, and on Axon guidance, Hippo, MAPK and Rap1 pathways. |
| Animal Protocol |
Animal/Disease Models: Female athymic nude mice using MIA PaCa-2 xenografts [1]
Doses: 1 mg/kg Route of Administration: intravenous (iv) (iv)injection; 1 mg/kg once or twice weekly; 28-day Experimental Results: Day 28 After several days, several animals had complete tumor regression with no obvious tumor regrowth. Animal/Disease Models: KPC mice with PDAC symptoms [1] Doses: 1 mg/kg Route of Administration: intravenous (iv) (iv)injection; 1 mg/kg, once a week; 3 consecutive weeks Experimental Results: Dramatically prolonged the survival of KPC mice, And the effect is better than gemcitabine. |
| References | |
| Additional Infomation |
G-Quadruplex-selective Transcription Inhibitor QN-302 is a naphthalene diimide (ND) derivative and selective G-quadruplex (G4) transcription inhibitor, with potential antineoplastic activity. Upon administration, QN-302 targets and binds to highly stable G-quadruplex DNA sequences that are prevalent within the promoter regions of cancer-related genes, thereby further stabilizing these complexes. This stabilization prevents unwinding and inhibits transcription factor binding, which leads to an inhibition of target gene transcription and expression and decreases G4-expressing cancer cell proliferation. Specifically, QN-302 downregulates the expression of the S100P gene in tumor cells. S100P, forming many quadruplex-forming sequences, plays a key role in the proliferation and motility pathways in several cancers and is upregulated in various tumor cell types. G4 sequences are over-represented in the promoter regions of many oncogenes.
|
| Molecular Formula |
C45H57N7O6
|
|---|---|
| Molecular Weight |
791.977391004562
|
| Exact Mass |
791.437
|
| CAS # |
2546091-70-5
|
| PubChem CID |
155318440
|
| Appearance |
Brown to reddish brown solid powder
|
| LogP |
1
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
58
|
| Complexity |
1800
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
OC1=C2C=C(C3C=CC(=CC=3)CN3CCCC3)C3C(N(CCCN4CCOCC4)C(C4=C/C(/C(C(N1CCCN1CCOCC1)=O)=C2C=34)=N\CCN1CCCC1)=O)=O
|
| InChi Key |
TZQVPFRBHPQZNM-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C45H57N7O6/c53-42-35-29-34(33-9-7-32(8-10-33)31-50-14-3-4-15-50)40-38-36(43(54)51(44(40)55)18-5-16-48-21-25-57-26-22-48)30-37(46-11-20-47-12-1-2-13-47)41(39(35)38)45(56)52(42)19-6-17-49-23-27-58-28-24-49/h7-10,29-30,53H,1-6,11-28,31H2
|
| Chemical Name |
14-hydroxy-6,13-bis(3-morpholin-4-ylpropyl)-10-(2-pyrrolidin-1-ylethylimino)-3-[4-(pyrrolidin-1-ylmethyl)phenyl]-6,13-diazatetracyclo[6.6.2.04,16.011,15]hexadeca-1(14),2,4(16),8,11(15)-pentaene-5,7,12-trione
|
| 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 : ~200 mg/mL (~252.53 mM)
|
|---|---|
| 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 | 1.2627 mL | 6.3133 mL | 12.6266 mL | |
| 5 mM | 0.2525 mL | 1.2627 mL | 2.5253 mL | |
| 10 mM | 0.1263 mL | 0.6313 mL | 1.2627 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
