Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
Other Sizes |
|
Targets |
PI4KIIα 0.47 μM (IC50)
|
---|---|
ln Vitro |
At the G2-M phase, PI-273 (2 μM; 48 hours) inhibits the cell cycle[1]. All three Ras wild-type breast cancer cells (MCF-7, T-47D, and SK-BR-3) undergo cell apoptosis when exposed to PI-273 (2 μM) for 48 hours[1]. AKT signaling pathway suppression is possible with PI-273 (0.5-2 μM; for 3 days) in a dose- and time-dependent way[1]. Both MCF-7 and T-47D cell proliferation is inhibited in a time-dependent manner by PI-273 at 1 μM and 2 μM [1].
|
ln Vivo |
In MCF-7 xenografts, PI-273 (intraperitoneal injection; 25 mg/kg/day; 15 days) significantly inhibits the tumor weight and volume[1]. The absolute bioavailability of PI-273 is 5.1%[1]. Its half-lives are 0.411 hours for intravenous treatment and 1.321 hours for intragastric administration (0.5 mg/kg intravenously or 1.5 mg/kg intragastrically; 0.08-5 hours).
|
Cell Assay |
Cell Cycle Analysis[1]
Cell Types: MCF-7, T-47D, SK-BR-3, MDA-MB-231, SUM229PE, Hs 578T cells Tested Concentrations: 2 μM Incubation Duration: 48 hrs (hours) Experimental Results: Blocked the cell cycle at the G2-M phase. Apoptosis Analysis[1] Cell Types: MCF-7, T-47D, and SK-BR-3 cells Tested Concentrations: 2 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induced cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3. Western Blot Analysis[1] Cell Types: MCF-7 cells Tested Concentrations: 0.5, 1, 2 μM Incubation Duration: For 3 days Experimental Results: Suppressed the AKT signaling pathway in a dose- and time-dependent manner. |
Animal Protocol |
Animal/Disease Models: Eightweeks old male BALB/c nude mice with MCF-7 cell[1]
Doses: 25 mg/kg Route of Administration: intraperitoneal (ip)injection; daily; 15 days Experimental Results: Suppressed the tumor volume and weight in the MCF-7 xenografts. Animal/Disease Models: Male SD (Sprague-Dawley) rats[1] Doses: 0.5 mg/kg (intravenously (iv)) or 1.5 mg/kg (intragastrically (po)) (pharmacokinetic/PK Study) Route of Administration: intravenously (iv) or intragastrically (po); 0.08, 0.16, 0.33, 0.67, 1, 1.5, 2, 3 and 5 hrs (hours) Experimental Results: Has a half-life of 0.411 hrs (hours) for intravenous (iv)administration and 1.321 hrs (hours) for intragastric (po)administration, and the absolute bioavailability of PI-273 is 5.1 %. |
References |
Molecular Formula |
C16H16CLN3O2S2
|
---|---|
Molecular Weight |
381.900139808655
|
Exact Mass |
381.037
|
CAS # |
925069-34-7
|
PubChem CID |
17168969
|
Appearance |
Light yellow to yellow solid powder
|
LogP |
4.2
|
Hydrogen Bond Donor Count |
3
|
Hydrogen Bond Acceptor Count |
4
|
Rotatable Bond Count |
4
|
Heavy Atom Count |
24
|
Complexity |
498
|
Defined Atom Stereocenter Count |
0
|
SMILES |
O=C(C1C(CC)=C(C)SC=1NC(NC(C1C=CC(Cl)=CC=1)=O)=S)N
|
InChi Key |
MIERMBQDBLFAFW-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C16H16ClN3O2S2/c1-3-11-8(2)24-15(12(11)13(18)21)20-16(23)19-14(22)9-4-6-10(17)7-5-9/h4-7H,3H2,1-2H3,(H2,18,21)(H2,19,20,22,23)
|
Chemical Name |
2-[(4-chlorobenzoyl)carbamothioylamino]-4-ethyl-5-methylthiophene-3-carboxamide
|
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 : 6.02 mg/mL (15.76 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 | 2.6185 mL | 13.0924 mL | 26.1849 mL | |
5 mM | 0.5237 mL | 2.6185 mL | 5.2370 mL | |
10 mM | 0.2618 mL | 1.3092 mL | 2.6185 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.