| ln Vitro |
Dalifab (5-500 nM; 7 days) can enhance the antiproliferative activity of anti-VEGFR TKIs in primary umbilical vein endothelial cells[1]. Dalifab (250 nM; 96 hours) combined with anti-VEGFR TKIs (axitinib, lenvatinib, or cabozantinib) can significantly increase the apoptosis level of HUVEC cells, which is superior to the use of either drug alone[1].
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| ln Vivo |
Dalifab (10 mg/kg; orally; twice daily; for 42 days) monotherapy can induce tumor growth arrest, and when combined with anti-VEGFR TKIs, it can achieve durable tumor regression in the Caki1 renal cell carcinoma xenograft model [1]. Dalifab (20 mg/kg, for KI-12-0073; orally; twice daily; for 28-31 days) can enhance the tumor growth inhibition mediated by cabozantinib and induce tumor cell cycle arrest in various renal cell carcinoma xenograft models. Combined therapy can significantly reduce tumor angiogenesis and achieve durable tumor regression [1].
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| Animal Protocol |
Animal/Disease Models:BALB/c nude mice [1]
Doses: 10 mg/kg Route of Administration: Oral; twice daily; 42 days Experimental Results: Tumor arrest was induced, with the mean percentage change in tumor volume approaching 0% on day 42. When used in combination with axitinib, lenvatinib or cabozantinib, durable tumor regression was achieved, with the mean percentage change in tumor volume reaching a negative value (tumor shrinkage) on day 42. Animal/Disease Models: BALB/c nude mice; NOD/SCID mice (for KI-12-0097 PDX) [1] Doses: 20 mg/kg (KI-12-0073 PDX) Route of Administration: Oral; twice daily; 28-31 days Experimental Results: When used in combination with cabozantinib, it enhanced tumor growth inhibition in all tested models and induced tumor regression in 4 out of 6 models. In the KI-12-0073 PDX model, it resulted in faster and more durable tumor regression compared to cabozantinib. After 14 days of treatment, it significantly reduced the area of CD31-positive endothelial cells and NG2-positive pericytes in KI-12-0073 tumors compared to cabozantinib. |
| References |
| CAS # |
3065226-39-0
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|---|---|
| Appearance |
Typically exists as solids at room temperature
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| Synonyms |
KO-2806
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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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