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| 10mg |
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| Targets |
SRX3177 targets multiple proteins involved in cancer cell growth and survival. It inhibits CDK4/6 (cyclin-dependent kinases 4 and 6), PI3K (phosphoinositide 3-kinase), and BRD4 (bromodomain-containing protein 4). By inhibiting these targets, the compound blocks cell cycle progression, PI3K/AKT/mTOR signaling, and epigenetic regulation. The compound has broad cytotoxic activity against cancer cells but is friendly to normal epithelial cells.
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| ln Vitro |
In cell-free biochemical assays, SRX3177 inhibits CDK4/6, PI3K, and BRD4 with potent IC50 values. These activities demonstrate the compound's direct inhibition of these targets. The compound's multi-target inhibition profile makes it a promising candidate for cancer therapy. The compound has broad cytotoxic activity against cancer cells but is friendly to normal epithelial cells.
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| ln Vivo |
In cell-based assays, SRX3177 exhibits broad cytotoxic activity against cancer cells but is friendly to normal epithelial cells. The compound's multi-target inhibition leads to potent anti-proliferative effects in various cancer cell lines. By inhibiting CDK4/6, PI3K, and BRD4, the compound blocks cell cycle progression, survival signaling, and epigenetic regulation. The compound has potential anticancer activity.
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| Enzyme Assay |
The cell-free assay for SRX3177 involves measuring the inhibition of CDK4/6, PI3K, and BRD4 activities. CDK4/6 inhibition is assessed using in vitro kinase assays with purified CDK4/6-cyclin complexes. PI3K inhibition is assessed using in vitro kinase assays with purified PI3K isoforms. BRD4 inhibition is assessed using binding assays with purified BRD4 bromodomains. The IC50 values are determined from dose-response curves.
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| Cell Assay |
Cell-based assays for SRX3177 involve culturing cancer cell lines and treating them with the compound at concentrations ranging from 0.001 to 10 μM. Cells are incubated for 48-72 hours, and cell viability is assessed using MTT or CCK-8 assays. The compound's effects on cell cycle progression, PI3K/AKT/mTOR signaling, and BRD4-mediated gene expression are assessed by flow cytometry and Western blotting. The compound's selectivity for cancer cells over normal cells is evaluated.
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| Animal Protocol |
In animal models, SRX3177 has been evaluated for its anti-tumor activity. Typical studies involve administration of the compound to tumor-bearing mice via oral or intraperitoneal routes at doses determined from toxicity studies. Tumor volumes are measured, and tissues are collected for analysis of CDK4/6, PI3K, and BRD4 inhibition. Efficacy is assessed by tumor growth inhibition. The compound's selectivity for cancer cells over normal cells suggests a potentially favorable therapeutic index.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SRX3177 have not been extensively reported. As a small molecule with a molecular weight of 584.69 g/mol, the compound would be expected to have moderate oral bioavailability and tissue penetration. The compound is typically stored at -20°C for 3 years in powder form. Further pharmacokinetic studies would be required to determine plasma half-life, clearance, and metabolic pathways.
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| Toxicity/Toxicokinetics |
SRX3177 is intended for research use only and lacks established toxicity profiles for therapeutic applications. Standard laboratory safety precautions should be observed when handling this chemical reagent. As a multi-target kinase and BRD4 inhibitor, the compound may have effects on normal cells as well as cancer cells. However, it has been reported to be friendly to normal epithelial cells. Standard toxicity studies in rodents would be required to determine the safety profile.
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| References | |
| Additional Infomation |
SRX3177 is a research-grade compound supplied for cancer research. It is not an approved pharmaceutical and has no clinical trial history. The compound is a potent triple inhibitor targeting CDK4/6, PI3K, and BRD4. It has broad cytotoxic activity against cancer cells but is friendly to normal epithelial cells. This product is intended for research use only.
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| Molecular Formula |
C31H32N6O4S
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| Molecular Weight |
584.688585281372
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| Exact Mass |
584.22
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| CAS # |
2241237-51-2
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| PubChem CID |
153289441
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| Appearance |
Light yellow to brown solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
42
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| Complexity |
1020
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(NC2=CC=C(C3C4OC(N5CCOCC5)=CC(=O)C=4SC=3)C=C2)=NC=C2C=C(C(N(C)C)=O)N(C3CCCC3)C2=N1
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| InChi Key |
XJKTXWSMMWPNTP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H32N6O4S/c1-35(2)30(39)24-15-20-17-32-31(34-29(20)37(24)22-5-3-4-6-22)33-21-9-7-19(8-10-21)23-18-42-28-25(38)16-26(41-27(23)28)36-11-13-40-14-12-36/h7-10,15-18,22H,3-6,11-14H2,1-2H3,(H,32,33,34)
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| Chemical Name |
7-cyclopentyl-N,N-dimethyl-2-[4-(5-morpholin-4-yl-7-oxothieno[3,2-b]pyran-3-yl)anilino]pyrrolo[2,3-d]pyrimidine-6-carboxamide
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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 | 1.7103 mL | 8.5515 mL | 17.1031 mL | |
| 5 mM | 0.3421 mL | 1.7103 mL | 3.4206 mL | |
| 10 mM | 0.1710 mL | 0.8552 mL | 1.7103 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
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