| Targets |
SIRT1 80.52 μM (IC50) SIRT2 92.21 μM (IC50) SIRT6 7.46 μM (IC50) HDAC3 111.9 μM (IC50) HDAC6 96.77 μM (IC50) HDAC8 102 μM (IC50)
|
|---|---|
| ln Vitro |
SiRT6-IN-3 (25 μM, 48 h) causes apoptosis and cell cycle arrest in PDAC [1]. By blocking cell signaling pathways, SIRT6-IN-3 (25 μM, 72 hours) prevents pancreatic cancer cells from proliferating [1].
|
| ln Vivo |
In tumor animal models, SIRT6-IN-3 (HY-156027; 20 mg/kg, intraperitoneal injection; once every two days for four weeks) exhibits anti-tumor properties [1]. Combining SIRT6-IN-3 (HY-156027; 20 mg/kg, intraperitoneal injection; once every two days for four weeks) with gemcitabine (ratio 2:1) amplifies the antitumor impact of the former [1].
|
| Cell Assay |
Apoptosis Analysis[1]
Cell Types: PDAC cells Tested Concentrations: 0, 6.25, 12.5, 25 μM Incubation Duration: 48 h Experimental Results: Increased the percentages of the G0-G1 phase and diminished cyclin D1 expression in a dose-dependent manner. Western Blot Analysis[1] Cell Types: PDAC cells Tested Concentrations: 0, 6.25, 12.5, 25 μM Incubation Duration: Overnight Experimental Results: Dramatically down-regulated p-mTOR, p-P70S6K, p-AKT, and p-ERK. Inhibited the activity of both mTORC1 and mTORC2. Dramatically up-regulated the expression of cleaved-PARP, cleaved-Caspase3, and cleaved-Caspase9. |
| Animal Protocol |
Animal/Disease Models: Tumor mouse model[1]
Doses: 20 mg/kg (in combination with 10 mg/kg gemcitabine) Route of Administration: intraperitoneal (ip)injection; Once every 2 days for 4 weeks Experimental Results: Inhibited the tumor mass 71.3% in mice with combinations of gemcitabine. Greatly increased the expression of apoptosis maker. |
| References |
| Exact Mass |
671.947
|
|---|---|
| CAS # |
3023471-40-8
|
| PubChem CID |
168510470
|
| Appearance |
Light yellow to yellow solid powder
|
| Hydrogen Bond Donor Count |
2
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
32
|
| Complexity |
561
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JGXUMUHLFCAFIT-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C21H29Br2N6S.BrH.ClH/c1-27(2)21(28(3)4)30-12-8-6-5-7-11-29-14-25-19-17(29)9-10-24-18(19)16-13-15(22)20(23)26-16;;/h9-10,13-14,26H,5-8,11-12H2,1-4H3;2*1H/q+1;;/p-1
|
| Chemical Name |
[6-[4-(4,5-dibromo-1H-pyrrol-2-yl)imidazo[4,5-c]pyridin-1-yl]hexylsulfanyl-(dimethylamino)methylidene]-dimethylazanium;bromide;hydrochloride
|
| 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.) |
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.
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