| ln Vitro |
CDK6-IN-2 (compound C32) (72 hours) selectively inhibited the viability of triple-negative breast cancer (TNBC) and BRCA1 mutant breast cancer cells with an IC50 value ≤0.08 μM, while exhibiting low activity against normal breast epithelial cells and estrogen receptor-positive (ER-positive) breast cancer cells [1]. CDK6-IN-2 (0-0.2 μM; 0-72 hours) effectively inhibited the proliferation and migration of MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells and induced apoptosis, cell cycle arrest, and intracellular reactive oxygen species (ROS) accumulation [1]. CDK6-IN-2 (0-0.20 μM; 72 hours) induced mitochondrial damage and dysfunction in MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells, including decreased membrane potential and structural abnormalities [1]. CDK6-IN-2 (0-0.20 μM; 72 h) inhibited autophagy flux and degradation processes in MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells, as evidenced by the co-accumulation of LC3II and P62 proteins [1].
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| ln Vivo |
CDK6-IN-2 (10-20 mg/kg; intraperitoneal injection; daily; 18 days) dose-dependently inhibited the growth of MDA-MB-231 tumors in BALB/c nude mice [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: Triple-negative breast cancer (TNBC) cell lines MDA-MB-231, MDA-MB-468, BT-549; BRCA1 mutant cell line MDA-MB-436; ER positive cell line MCF-7; normal breast epithelial cell line MCF-10A Tested Concentrations: / Incubation Duration: 72 hours Experimental Results: Selectively inhibited the viability of TNBC and BRCA1 mutant breast cancer cells, with IC50 values of 0.06 μM (MDA-MB-231), 0.08 μM (MDA-MB-468), 0.04 μM (BT-549) and 0.06 μM (MDA-MB-436), respectively. The activity against non-TNBC cells was reduced, with IC50 values of 0.39 μM (MCF-7) and 2.30 μM (MCF-10A), respectively. |
| Animal Protocol |
Animal/Disease Models:BALB/c nude mice (female, 4 weeks old, subcutaneously inoculated with 1×10⁷ MDA-MB-231 cells)[1]
Doses: 10 mg/kg; 20 mg/kg Route of Administration: Intraperitoneal injection; once daily for 18 days Experimental Results: The average tumor weight decreased to 0.68 g (10 mg/kg group) and 0.23 g (20 mg/kg group), respectively, significantly lower than the 1.45 g in the control group. The counts of Ki67, CDK6 and RB1 positive cells in the tumor tissue of the treatment group were significantly downregulated. The counts of Cleaved Caspase-3 positive cells in the tumor tissue of the treatment group were significantly upregulated. There was no significant change in mouse body weight. H&E staining showed no pathological damage in the major organs (heart, liver, spleen, lung and kidney). |
| References |
| Appearance |
Typically exists as solids 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.) |
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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