| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
IKP-104 (0-25 μM) can inhibit tau-induced polymerization of ungraded tubulin and homologous αβII and αβIV, but has no effect on αβIII[1]. IKP-104 (1.5 μM) can force a large number of pre-formed microtubules to form aggregates (ungraded tubulin and αβIII) and spirochetes (αβII isoform), but has no effect on the morphology of microtubules formed by αβIV[1]. KP-104 (0-40 μM, 0-40 min) can increase absorbance and change the formation of aggregates and the morphology of existing microtubules[1]. KP-104 is cytotoxic to L1210, B16, Lewis, K562 and HeLa cells, with IC50 values of 0.0025, 5.2, 0.0017, 0.0012 and 0.015 μg/mL, respectively[2]. KP-104 (3.6 μg/mL, 0-48 hours) increases the proportion of round cells by inhibiting the polymerization of cytoskeleton microtubules in B16 cells and inducing the depolymerization of microtubules, thereby arresting cells in the M phase and mitotic phase [2][3].
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|---|---|
| ln Vivo |
IKP-104 (0.5-5 mg/kg, intraperitoneal/subcutaneous injection, once daily for 5-9 days) showed antitumor activity in mouse ascites tumor and mouse Lewis lung cancer models [2].
|
| Cell Assay |
Cell Cycle Analysis[2][3]
Cell Types: B16 cells Tested Concentrations: 3.6 μg/mL Incubation Duration: 0, 1, 3, 6, 9, 12, 24 and 48 h Experimental Results: Increased the proportion of round-shaped cells, arrested cells in G1-M phase, and induced polyploid and multinuclear. Accumulated mitotic cells, and the Ml. Caused the fine reticular microtubule network of prophase cells to disappear, resulting in a single mitotic spindle during metaphase, shortened the centromere microtubules during anaphase and telophase, and the early interphase microtubule network to re-form after cell division. Depolymerized spindle microtubules in mitotic cells, but no changes in the microtubule network were observed in interphase cells after 20 minutes of exposure. Caused the microtubule network of interphase cells to gradually disappear after 2 h of treatment, weak fluorescence appears in the cytoplasm of mitotic and interphase cells, accompanied by a small amount of microtubule fragments. Resulted the induction of bundles of varying sizes composed of numerous wavy protofilaments at 2 and 24 h. |
| Animal Protocol |
Animal/Disease Models: CDF1 murine ascetic tumor (L1210, 1x105) model[2]
Doses: 0.5 mg/kg, 1 mg/kg, 5 mg/kg Route of Administration: i.p., once a day, 5 days Experimental Results: Showed antitumor activity, at doses of 1.0 and 5.0 mg/kg showed effects com-parable to those of 5-Fluorouracil at 10.0 and 20.0 mg/kg andvindesine at 0.3 mg/kg. Animal/Disease Models: C57BL/6 murine Lewis (1x105) lung carcinoma model[2] Doses: 1 mg/kg, 5 mg/kg Route of Administration: s.c., once a day, 9 days Experimental Results: Showed antitumor activity. |
| References |
| Molecular Formula |
C26H21CLFNO3
|
|---|---|
| Molecular Weight |
449.90
|
| CAS # |
114231-14-0
|
| Appearance |
Typically exists as solids at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.2227 mL | 11.1136 mL | 22.2272 mL | |
| 5 mM | 0.4445 mL | 2.2227 mL | 4.4454 mL | |
| 10 mM | 0.2223 mL | 1.1114 mL | 2.2227 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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