| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 1g | |||
| Other Sizes |
| Targets |
P-2281 targets the mechanistic target of rapamycin (mTOR). mTOR is a key protein kinase that regulates cell growth, proliferation, and metabolism. By inhibiting mTOR, P-2281 disrupts downstream signaling pathways that promote cell growth and survival. This inhibition contributes to its anticancer and anti-inflammatory effects.
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|---|---|
| ln Vitro |
P-2281 is an mTOR inhibitor. It inhibits mTOR activity in colon cancer cells. Its activity has been confirmed in various in vitro assays. It suppresses dextran sulfate sodium (DSS)-induced colitis by inhibiting T cell function.
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| ln Vivo |
P-2281 is efficacious in a murine model of human colitis. It significantly inhibits DSS-induced weight loss, improves rectal bleeding index, decreases disease activity index, and reverses DSS-induced shortening of the colon. These effects demonstrate its in vivo anti-inflammatory efficacy.
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| Enzyme Assay |
The primary in vitro assays for P-2281 include mTOR kinase activity assays, where the enzyme is incubated with a substrate and the compound, and the phosphorylation of the substrate is measured. Its ability to inhibit mTOR activity in cancer cells is assessed in cellular assays.
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| Cell Assay |
Cellular assays for P-2281 involve treating colon cancer cells or T cells with the compound and measuring its effects on mTOR signaling, cell proliferation, and T cell function. The inhibition of mTOR and downstream targets, such as p70S6K and 4E-BP1, is assessed by Western blot. T cell proliferation and function are assessed in functional assays.
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| Animal Protocol |
In vivo animal experiments for P-2281 have been conducted using the dextran sulfate sodium (DSS) model of colitis in mice. P-2281 was administered to mice, and its effects on disease activity index, weight loss, rectal bleeding, and colon length were assessed. The compound significantly inhibited colitis symptoms.
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| ADME/Pharmacokinetics |
P-2281 has a molecular weight of 209.63 g/mol and a molecular formula of C9H8ClN3O. It is a small molecule that is typically used as a research reagent. Its purity is typically ≥98%. The compound is an mTOR inhibitor with anticancer and anti-inflammatory properties.
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| Toxicity/Toxicokinetics |
The toxicological profile of P-2281 is not extensively detailed in the provided sources. As a research compound, it is not intended for human use. Standard safety precautions should be followed when handling. Its safety would need to be established through preclinical studies if it were to be developed for therapeutic applications.
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| References | |
| Additional Infomation |
mTOR inhibitor; structure can be found in the first article.
P-2281 is an mTOR inhibitor with anticancer and anti-inflammatory properties. It inhibits mTOR activity in colon cancer cells and suppresses DSS-induced colitis in a murine model. It is efficacious in a murine model of human colitis. P-2281 is available from various chemical suppliers for research purposes. |
| Molecular Formula |
C9H8CLN3O
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|---|---|
| Molecular Weight |
209.632320404053
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| Exact Mass |
209.035
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| Elemental Analysis |
C, 51.57; H, 3.85; Cl, 16.91; N, 20.05; O, 7.63
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| CAS # |
1112994-35-0
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| Related CAS # |
1112994-35-0;
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| PubChem CID |
25141337
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| Appearance |
White to off-white solid powder
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| LogP |
1.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
260
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC(C)C(NC1C=NC(C#N)=CC=1)=O
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| InChi Key |
VFOLQYOVUCHHET-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H8ClN3O/c1-6(10)9(14)13-8-3-2-7(4-11)12-5-8/h2-3,5-6H,1H3,(H,13,14)
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| Chemical Name |
2-chloro-N-(6-cyanopyridin-3-yl)propanamide
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| Synonyms |
P 2281; P2281; P-2281
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| HS Tariff Code |
2934.99.9001
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| 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)
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| 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
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|---|---|
| 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 | 4.7703 mL | 23.8515 mL | 47.7031 mL | |
| 5 mM | 0.9541 mL | 4.7703 mL | 9.5406 mL | |
| 10 mM | 0.4770 mL | 2.3852 mL | 4.7703 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.
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