| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
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| Other Sizes |
|
| Targets |
tumor-associated macrophages (TAMs)[1]
|
|---|---|
| ln Vitro |
Antitumor agent-19 (Compound 23a; 10-50 µM; 1 hour; RAW 264.7 cells) successfully promotes the expression of M1-phenotype macrophage markers (IL-1β, TNF-α, iNOS, and IL-12α) in RAW 264.7 cells in a dose-dependent manner over the course of an hour. It has been observed that antitumor agent-19 repolarizes TAMs from M1 (anti-tumor) and M2 (pro-tumor) in a dose-dependent manner[1].
|
| ln Vivo |
The LLC mouse model's tumor growth can be significantly inhibited by antitumor agent-19 (Compound 23a; 5 mg/kg; intraperitoneal injection; every other day; for 30 days; C57BL/6 female mice). Furthermore, the combined use of anti-PD-1 antibody and antitumor agent-19 provides more potent antitumor effects than using either one alone in vivo[1].
|
| Cell Assay |
RT-PCR[1]
Cell Types: RAW 264.7 cells Tested Concentrations: 10 µM, 20 µM, or 50 µM Incubation Duration: 1 hour Experimental Results: Induced the expression of M1-phenotype macrophage markers (IL-1β, TNF-α, iNOS and IL-12α) in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Six-to eightweeks old C57BL/6 female mice with lewis lung cancer cells (LLC)[1]
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection; every other day; for 30 days Experimental Results: Remarkably inhibited tumor growth of the LLC mouse model. |
| References |
[1]. Pei H, et al. iscovery of potent ureido tetrahydrocarbazole derivatives for cancer treatments through targeting tumor-associated macrophages. Eur J Med Chem. 2019 Sep 28;183:111741.
|
| Molecular Formula |
C24H21CLF3N5O
|
|---|---|
| Molecular Weight |
487.90465426445
|
| Exact Mass |
487.138
|
| CAS # |
2379727-90-7
|
| PubChem CID |
139600306
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
5
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
34
|
| Complexity |
742
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
RTILPKXOEYEQSE-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C24H21ClF3N5O/c1-33-12-13(11-29-33)16-3-2-4-21-22(16)17-9-14(6-8-20(17)32-21)30-23(34)31-15-5-7-19(25)18(10-15)24(26,27)28/h2-5,7,10-12,14,32H,6,8-9H2,1H3,(H2,30,31,34)
|
| Chemical Name |
1-[4-chloro-3-(trifluoromethyl)phenyl]-3-[5-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl]urea
|
| 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 | 2.0496 mL | 10.2480 mL | 20.4960 mL | |
| 5 mM | 0.4099 mL | 2.0496 mL | 4.0992 mL | |
| 10 mM | 0.2050 mL | 1.0248 mL | 2.0496 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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