| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
CCT129957 targets phospholipase C-γ (PLC-γ). PLC-γ is a key enzyme in the phosphoinositide signaling pathway that hydrolyzes phosphatidylinositol 4,5-bisphosphate (PIP2) into inositol 1,4,5-trisphosphate (IP3) and diacylglycerol (DAG). IP3 triggers the release of calcium from intracellular stores, while DAG activates protein kinase C (PKC). By inhibiting PLC-γ, CCT129957 disrupts this signaling cascade, thereby modulating calcium mobilization and downstream cellular responses.
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| ln Vitro |
In addition to lipophilic contacts, the projected binding mechanism of CCT129957 has a mature hydrogen bonding pattern [1]. Renal UO-31 and mammary T-47D development is inhibited by CCT129957 by approximately 60-70%[2].
CCT129957 is a potent PLC-γ inhibitor with an IC50 of approximately 3 μM. It has been shown to inhibit Ca2+ release in squamous carcinoma cells at approximately 15 μM. The compound also exhibits anticancer activity. Its ability to modulate calcium signaling makes it a useful tool for studying the role of PLC-γ in various cellular processes, including cell proliferation, migration, and survival. |
| ln Vivo |
Specific in vivo activity data for CCT129957 is not extensively detailed in the available literature. As a research compound, its in vivo effects are primarily studied in the context of PLC-γ inhibition and its impact on cancer cell biology. Further studies are needed to fully characterize its in vivo efficacy and pharmacokinetic properties.
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| Enzyme Assay |
CCT129957's activity as a PLC-γ inhibitor is assessed using in vitro enzyme assays that measure its ability to inhibit PLC-γ enzymatic activity. These assays typically involve measuring the hydrolysis of PIP2 or the production of IP3. The IC50 of approximately 3 μM is determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for CCT129957 involve treating cancer cell lines with the compound and measuring its effects on calcium signaling and cell viability. Calcium release can be measured using fluorescent calcium indicators such as Fura-2 or Fluo-4. The compound's antiproliferative effects can be assessed using cell viability assays such as MTT or CellTiter-Glo.
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| Animal Protocol |
In vivo animal model protocols for CCT129957 would involve its administration to tumor-bearing mice to evaluate its antitumor efficacy. The compound's effects on tumor growth and calcium signaling in tumor tissues would be assessed. Specific protocols are not detailed in the available literature.
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| ADME/Pharmacokinetics |
CCT129957 has a molecular weight of 309.32 and a molecular formula of C17H15N3O3. It is soluble in DMSO at 100 mg/mL (323.29 mM). The compound is stored at -20°C and is stable for at least 2 years. Specific pharmacokinetic data is not extensively detailed in the available literature.
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| Toxicity/Toxicokinetics |
Specific toxicological data for CCT129957 is not extensively detailed in the available literature. As a research compound, it is intended for research use only and not for human consumption. Standard safety assessments would be required for clinical development.
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| References | |
| Additional Infomation |
CCT129957 (CAS# 883098-58-6) is a research compound used to study PLC-γ function and calcium signaling. It is an indole derivative and a potent PLC-γ inhibitor with an IC50 of approximately 3 μM. It has a molecular weight of 309.32 and a molecular formula of C17H15N3O3. It is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C17H15N3O3
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|---|---|
| Molecular Weight |
309.319303750992
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| Exact Mass |
309.111
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| Elemental Analysis |
C, 66.01; H, 4.89; N, 13.58; O, 15.52
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| CAS # |
883098-58-6
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| PubChem CID |
2823659
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
431
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)CCNC(=O)C2=CC3=C(N2)C(=CC=C3)[N+](=O)[O-]
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| InChi Key |
VXDJRTJBOJFUOC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H15N3O3/c21-17(18-10-9-12-5-2-1-3-6-12)14-11-13-7-4-8-15(20(22)23)16(13)19-14/h1-8,11,19H,9-10H2,(H,18,21)
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| Chemical Name |
7-nitro-N-(2-phenylethyl)-1H-indole-2-carboxamide
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| Synonyms |
CCT-129957; CCT 129957; CCT129957
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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) |
DMSO : ~100 mg/mL (~323.29 mM)
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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 | 3.2329 mL | 16.1645 mL | 32.3290 mL | |
| 5 mM | 0.6466 mL | 3.2329 mL | 6.4658 mL | |
| 10 mM | 0.3233 mL | 1.6164 mL | 3.2329 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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