Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
CDK4 10 nM (IC50) CDK6 16 nM (IC50) CDK1 >10000 nM (IC50) CDK2 1045 nM (IC50) CDK7 2595 nM (IC50) CDK9 2664 nM (IC50)
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ln Vitro |
Compound 42, CDK4/6-IN-14 (1-6 μM; 5 days) has strong anti-proliferative effects on the breast cancer cell lines MCF-7, T47D, and ZR-75-1. MCF-7 and T47D cell proliferation and clone formation are markedly inhibited by CDK4/6-IN-14[1]. In a dose-dependent manner, CDK4/6-IN-14 (compound 42; 1-6 μM) stops the cell cycle at the G1 phase in MCF-7 and T47D cells[1]. Compound 42, CDK4/6-IN-14, effectively reduces retinoblastoma (RB) phosphorylation at 1-6 μM for 24 hours, without significantly altering RB protein production. Moreover, CDK4/6-IN-14 has a concentration-dependent influence on cyclin D1 and c-MYC levels[1].
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ln Vivo |
CDK4/6-IN-14 (compound 42; 100-150 mg/kg; po; once daily; for 23 days) dramatically suppresses the MCF-7 xenograft model's ability to grow tumors[1]. Compound 42, CDK4/6-IN-14, has an appropriate t1/2 for both oral and intravenous administration (2.62 and 3.59 hours, respectively). Additionally, CDK4/6-IN-14 has an oral bioavailability of 43%[1]. Sprague-Dawley rats' pharmacokinetic parameters for CDK4/6-IN-14 (Compound 42)[1]. administrator. The dose is as follows: IV 290.52 372.56 3.50 0.033 2.62 PO 144.11 1612.18 9.11 6 3.59 43 Cmax (ng/mL) AUC0-∞ (h × ng/mL) MRT0-∞ (h) Tmax (h) t1/2 (h) F (%)
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Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: MCF-7 and T47D cells Tested Concentrations: 1 μM, 2 μM, 4 μM (T47D cells); 1.5 μM, 3 μM, 6 μM (MCF-7 cells) Incubation Duration: 5 days Experimental Results: Dramatically inhibited growth and clone formation of MCF-7 and T47D cells. Western Blot Analysis[1] Cell Types: MCF-7 and T47D cells Tested Concentrations: 1 μM, 2 μM, 4 μM (T47D cells); 1.5 μM, 3 μM, 6 μM (MCF-7 cells) Incubation Duration: 24 hrs (hours) Experimental Results: Dramatically inhibited the phosphorylation of RB. |
Animal Protocol |
Animal/Disease Models: BALB/c nude mice bearing MCF-7 cells[1]
Doses: 100 mg/kg, 150 mg/kg Route of Administration: Orally administration; one time/day; for 23 days Experimental Results: Dramatically inhibited tumor growth of the MCF-7 xenograft model. |
References |
[1]. Weijiao Chen, et al. Discovery, Optimization, and Evaluation of Selective CDK4/6 Inhibitors for the Treatment of Breast Cancer. J Med Chem. 2022 Nov 24;65(22):15102-15122.
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Molecular Formula |
C24H27CLFN7O
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Molecular Weight |
483.97
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CAS # |
2699091-15-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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 | 2.0662 mL | 10.3312 mL | 20.6624 mL | |
5 mM | 0.4132 mL | 2.0662 mL | 4.1325 mL | |
10 mM | 0.2066 mL | 1.0331 mL | 2.0662 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.