| Size | Price | Stock | Qty |
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| 10mg |
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| Other Sizes |
| ln Vitro |
Treatment with YZ-836P (0–6 µM; 48 h) for 48 hours significantly reduced cell viability in HCC1806 (IC50 = 2.1 µM) and HCC1937 (IC50 = 1.0 µM) triple-negative breast cancer (TNBC) cell lines [1]. YZ-836P (0–10 µM; 48 h) and (4 µM; 0–72 h) reduced the expression levels of PRMT5 and KLF5 proteins in HCC1806 and HCC1937 TNBC cell lines in a dose- and time-dependent manner [1]. YZ-836P (0.25–1.00 µM; 2 days) inhibited colony formation in HCC1806 and HCC1937 TNBC cell lines in a concentration-dependent manner after an initial 2-day treatment [1]. YZ-836P (1–6 µM; 24 h) concentration-dependently inhibited DNA synthesis in HCC1806 and HCC1937 triple-negative breast cancer (TNBC) cell lines [1]. YZ-836P (2–6 µM; 48 h) concentration-dependently induced G1 phase cell cycle arrest in HCC1806 and HCC1937 TNBC cell lines [1]. YZ-836P (2–6 µM; 48 h) concentration-dependently regulated the expression of cell cycle-related proteins in HCC1806 and HCC1937 TNBC cell lines (decreased the expression of Cyclin D1, CDK4, and CDK6; increased the expression of p21 and p27) [1]. YZ-836P (2–6 µM; 48 h) concentration-dependently modulates the expression of apoptosis-related proteins in HCC1806 and HCC1937 triple-negative breast cancer (TNBC) cell lines (increasing the expression of cleaved PARP and cleaved Caspase 3; decreasing the expression of XIAP and Mcl-1) [1]. YZ-836P (2–6 µM; 48 h) concentration-dependently induces apoptosis in HCC1806 and HCC1937 TNBC cell lines [1]. YZ-836P (4 µM) directly binds to PRMT5, increasing its thermostability (CETSA assay) and decreasing its sensitivity to protease degradation (DARTS assay) [1]. YZ-836P (4 µM; 48 h) increases PRMT5 ubiquitination in HEK293T cells and promotes CRBN-dependent proteasome-mediated PRMT5 degradation [1]. Treatment with YZ-836P (0-10 µM; 48 hours) for 48 hours significantly reduced the viability of PDO-32 (IC50 = 2.072 µM) and PDO-33 (IC50 = 4.746 µM) organoids derived from TNBC patients [1].
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| ln Vivo |
YZ-836P (50 mg/kg; intraperitoneal injection; once every other day; for a total of 4 times) has strong in vivo antitumor activity against TNBC xenografts, can reduce tumor growth, and does not cause measurable systemic toxicity [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: HCC1806, HCC1937 triple-negative breast cancer (TNBC) cell lines Tested Concentrations: 0, 2, 4, 6 µM Incubation Duration: 48 hours Experimental Results: Significantly reduced the viability of HCC1806 and HCC1937 cells. The IC50 value was 2.1 µM in HCC1806 cells and 1.0 µM in HCC1937 cells. Western Blot Analysis [1] Cell Types: HCC1806, HCC1937 Triple Negative Breast Cancer (TNBC) Cell Lines Tested Concentrations: 0, 2, 4, 6, 8, 10 µM (concentration-dependent); 4 µM (time-dependent) Incubation Duration: 48 h (concentration-dependent); 0, 6, 12, 24, 48, 72 h (time-dependent) Experimental Results: Protein levels of PRMT5 and its downstream target KLF5 were significantly reduced in both cell lines. The reduction was concentration-dependent (0-10 µM, 48 h) and time-dependent (4 µM, 0-72 h). The protein level reduction could be detected as early as 6 h. Western Blot Analysis [1] Cell Types: HCC1806, HCC1937 triple-negative breast cancer cell lines Tested Concentrations: 0, 2, 4, 6 µM Incubation Duration: 48 hours Experimental Results: Concentration-dependently decreased the protein levels of Cyclin D1, CDK4, and CDK6 in both cell lines, and increased the levels of p21 and p27. Concentration-dependently promoted the increase of cleaved PARP and cleaved Caspase 3, and decreased the levels of the anti-apoptotic proteins XIAP and Mcl-1 in both cell lines. |
| Animal Protocol |
Animal/Disease Models:Nude mice (approximately 6 weeks old) [1]
Doses: 50 mg/kg Route of Administration: Intraperitoneal injection; once every other day; for a total of 4 times Experimental Results: Compared with the control group, tumor volume and weight were significantly reduced. The proportion of lysing Caspase 3 positive cells in the tumor tissue was significantly increased. Compared with the control group, there were no significant changes in mouse body weight, serum creatinine, alanine aminotransferase, or aspartate aminotransferase levels. |
| References |
| Molecular Formula |
C45H57N9O7
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|---|---|
| Molecular Weight |
835.99
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| CAS # |
3086041-35-9
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C1N(C2C(NC(CC2)=O)=O)C(C3=CC=C(NCCCCCCCCCC(N4CCC(CC4)NC5=NC=NC(C(NC[C@H](O)CN6CC7=CC=CC=C7CC6)=O)=C5)=O)C=C31)=O
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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 | 1.1962 mL | 5.9809 mL | 11.9619 mL | |
| 5 mM | 0.2392 mL | 1.1962 mL | 2.3924 mL | |
| 10 mM | 0.1196 mL | 0.5981 mL | 1.1962 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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