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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
TAM-IN-2 targets the TAM family of receptor tyrosine kinases, which includes Tyro3, Axl, and Mer. These receptors play critical roles in various cellular processes, including cell survival, proliferation, migration, and immune regulation. By inhibiting TAM receptors, TAM-IN-2 modulates downstream signaling pathways, such as PI3K/AKT and MAPK/ERK, which are involved in tumor progression and immune evasion. The compound is a valuable tool for studying TAM receptor biology.
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| ln Vitro |
In vitro, TAM-IN-2 acts as an inhibitor of TAM receptors. It is a pyrrolotriazine compound (0904) extracted from a patent. Its inhibitory activity on TAM receptors makes it a valuable tool for studying the role of these receptors in cancer cell proliferation, survival, and migration. The compound's effects on TAM receptor signaling and downstream pathways are typically assessed in cell-based assays measuring receptor phosphorylation and downstream signaling.
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| ln Vivo |
In vivo studies of TAM-IN-2 are likely focused on evaluating its antitumor efficacy and immunomodulatory effects in animal models. As a TAM receptor inhibitor, the compound is expected to inhibit tumor growth and enhance anti-tumor immune responses. TAM receptors are involved in immune regulation, and their inhibition can promote anti-tumor immunity. Further in vivo studies are needed to fully characterize its efficacy, safety, and pharmacokinetic profile.
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| Enzyme Assay |
For in vitro enzyme/receptor binding assays, TAM-IN-2 can be evaluated using kinase activity assays that measure TAM receptor kinase activity. The compound is incubated with recombinant Tyro3, Axl, or Mer kinase and ATP at various concentrations. Kinase activity is quantified by measuring phosphorylation of peptide substrates using radiometric, fluorescence-based, or ELISA methods. IC₅0 values are determined from dose-response curves. Selectivity profiling against other kinases may be performed to confirm specificity.
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| Cell Assay |
For in vitro cellular experiments, TAM-IN-2 is tested in cell lines expressing TAM receptors, such as cancer cell lines with high Axl or Mer expression. Cells are cultured in appropriate media and treated with various concentrations of the compound. TAM receptor phosphorylation and downstream signaling are assessed by Western blotting. Cell viability, proliferation, migration, and apoptosis are evaluated using standard assays. The compound's effects on immune cell function can be assessed in co-culture systems.
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| Animal Protocol |
For in vivo animal experiments, TAM-IN-2 can be administered to tumor-bearing mice via various routes, including oral gavage, intravenous injection, or intraperitoneal injection. Xenograft models using human cancer cell lines or syngeneic mouse tumor models are commonly used to evaluate antitumor efficacy and immunomodulatory effects. Typical dosing regimens may range from 1 to 50 mg/kg. Tumor volume, immune cell infiltration, and pharmacodynamic markers are measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of TAM-IN-2 are not extensively detailed in the provided references. As a small molecule with a molecular weight of 583.59, it may have reasonable oral bioavailability and tissue distribution. The compound is soluble in DMSO at 5 mg/mL. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies.
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| Toxicity/Toxicokinetics |
Toxicological data for TAM-IN-2 are limited, as it is primarily a research tool. As a TAM receptor inhibitor, its toxicity would depend on the importance of TAM receptors for normal cellular function and immune regulation. Comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and cardiotoxicity assessments would be needed for further development. Appropriate safety precautions should be taken when handling this compound.
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| References | |
| Additional Infomation |
TAM-IN-2 is a research compound used to study TAM receptor biology and evaluate TAM receptors as therapeutic targets. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound is extracted from patent US 20170275290 A1, pyrrolotriazine compound 0904.
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| Molecular Formula |
C31H27F2N7O3
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|---|---|
| Molecular Weight |
583.58799290657
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| Exact Mass |
583.214
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| CAS # |
2135642-56-5
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| PubChem CID |
130447757
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| Appearance |
White to off-white solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
43
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| Complexity |
1120
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=C(C=CC=1C1=C2C(N)=NC=NN2C(=C1)C1CCN(C(C)=O)CC1)NC(C1=CC=CN(C2C=CC(=CC=2)F)C1=O)=O
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| InChi Key |
PLCVJNJRUVNDEY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H27F2N7O3/c1-18(41)38-13-10-19(11-14-38)27-16-25(28-29(34)35-17-36-40(27)28)23-9-6-21(15-26(23)33)37-30(42)24-3-2-12-39(31(24)43)22-7-4-20(32)5-8-22/h2-9,12,15-17,19H,10-11,13-14H2,1H3,(H,37,42)(H2,34,35,36)
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| Chemical Name |
N-[4-[7-(1-acetylpiperidin-4-yl)-4-aminopyrrolo[2,1-f][1,2,4]triazin-5-yl]-3-fluorophenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide
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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) |
DMSO : ~5 mg/mL (~8.57 mM)
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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 | 1.7135 mL | 8.5677 mL | 17.1353 mL | |
| 5 mM | 0.3427 mL | 1.7135 mL | 3.4271 mL | |
| 10 mM | 0.1714 mL | 0.8568 mL | 1.7135 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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