| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ROR1-IN-4 (Compound 59) (72 h) showed potent antiproliferative activity (IC50 = 0.075 μM) in the triple-negative breast cancer (TNBC) cell line MDA-MB-231, but no significant antiproliferative activity in the non-triple-negative breast cancer cell lines MCF-7 (IC50 > 10 μM) and HEK-293T (IC50 = 9.72 μM) [1]. ROR1-IN-4 (0.1-3 μM, 48 h) induced apoptosis in MDA-MB-231 cells and inhibited phosphorylation of ROR1 (Tyr786) [1]. ROR1-IN-4 (0.1-1 μM, 14 days) reduced colony formation in MDA-MB-231 cells [1].
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|---|---|
| ln Vivo |
ROR1-IN-4 (Compound 59) (10-20 mg/kg, ip, once a week, 30 days) showed good antitumor activity in nude mice with MDA-MB-231 subcutaneous xenografts [1]. ROR1-IN-4 (10 mg/kg, ip, once a week, 45 days) showed potent antitumor growth and antimetastatic effects in nude mice with MDA-MB-231-Luc orthotopic breast xenografts [1].
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: MDA-MB-231 cells Tested Concentrations: 0.1, 0.3, 1 μM Incubation Duration: 48 h Experimental Results: Induced apoptosis in MDA-MB-231 cells. Reduced the expression of anti-apoptotic protein Bcl-2. Increased the expression of pro-apoptotic protein Bax, and promotes the cleavage of PARP in a concentration-dependent manner. |
| Animal Protocol |
Animal/Disease Models: MDA-MB-231 cells (5 × 106 in 100 µL mixture of PBS and Matrigel at 1:1 ratio) were subcutaneously implanted into the flanks of 4-5-week-old female BALB/c nude mice to establish the subcutaneous TNBC xenograft model[1]
Doses: 10, 20 mg/kg Route of Administration: i.p. every other day for 30 days Experimental Results: Achieved tumor growth inhibition (TGI) rates of 62.1% and 92.1% at doses of 10 mg/kg and 20 mg/kg, respectively. Showed no significant decrease in body weight of nude mice during the 30-day administration period. Led to no significant histopathological changes in major organs (heart, liver, spleen, lung, kidney) of nude mice. Resulted in no increase in tumor size of nude mice in the 20 mg/kg dose group throughout the entire administration period. Animal/Disease Models: MDA-MB-231-Luc cells (3 × 106) were orthotopically implanted into the mammary fat pads of 4-5-week-old female BALB/c nude mice to establish the orthotopic breast TNBC xenograft model[1] Doses: 10 mg/kg Route of Administration: i.p. every other day for 45 days Experimental Results: Significantly reduced the size of orthotopic breast tumors in nude mice. Inhibited tumor metastasis effectively: no tumor metastasis was found in nude mice at the 45th day of treatment. Caused no obvious pathological changes in the heart and kidneys of nude mice; only mild inflammatory cell infiltration was observed in the liver, and the degree of spleen lesions and tumor cell invasion was lower than that in the vehicle group. Delayed the occurrence of mouse death. Showed no significant abnormal changes in the body weight. |
| References |
| Molecular Formula |
C29H30F2N6O
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|---|---|
| Molecular Weight |
516.58
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| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9358 mL | 9.6790 mL | 19.3581 mL | |
| 5 mM | 0.3872 mL | 1.9358 mL | 3.8716 mL | |
| 10 mM | 0.1936 mL | 0.9679 mL | 1.9358 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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