| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
RET kinase. RET-IN-7 is a RET inhibitor that exerts its effects by binding to the ATP-binding site of the kinase, thereby preventing ATP from binding and activating downstream signaling pathways.
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|---|---|
| ln Vitro |
RET-IN-7 demonstrates potent in vitro RET kinase inhibition. It effectively inhibits the activity of the RET enzyme, disrupting its signaling cascade. This leads to a strong antiproliferative effect in RET-driven cancer cell lines in culture.
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| ln Vivo |
In mouse xenograft models of RET-driven tumors, RET-IN-7 shows robust in vivo efficacy. Following multiday dosing in mice, it significantly inhibits tumor growth. This confirms its potential as an effective in vivo tool for studying the role of RET in cancer progression.
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| Enzyme Assay |
Cell-free RET kinase activity assays are performed using a recombinant RET enzyme, a peptide substrate, and ATP. The compound is incubated with the enzyme for 30-60 minutes, and the level of substrate phosphorylation is measured using a luminescence-based detection system (e.g., ADP-Glo). The IC50 is calculated from dose-response curves.
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| Cell Assay |
RET-dependent cancer cell lines are seeded in 96-well plates and cultured overnight. The next day, cells are treated with a range of RET-IN-7 concentrations for 72 hours. Cell viability is then measured using the MTT assay or CellTiter-Glo reagent, and the IC50 is determined by nonlinear regression analysis.
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| Animal Protocol |
To assess in vivo efficacy, a RET-driven tumor xenograft model is established in immunodeficient mice. When tumors reach a predetermined size, mice are randomized into treatment and control groups. RET-IN-7 is administered by oral gavage once daily. Tumor volumes are measured with calipers twice weekly, and body weight is monitored as an indicator of toxicity.
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| ADME/Pharmacokinetics |
Limited pharmacokinetic data are available. The molecular weight of RET-IN-7 is 458.92, with a formula of C22H24ClFN6O2. It is soluble in DMSO (16.67 mg/mL). For in vivo studies, the compound is typically formulated in a suitable vehicle such as 0.5% methylcellulose or a DMSO/PEG300/Tween 80/saline mixture.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported. RET-IN-7 is a research compound, and its toxicity profile has not been fully characterized in publicly available literature. As a selective RET inhibitor, its safety profile is expected to be based on the pharmacological inhibition of its target, with potential on-target effects.
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| References | |
| Additional Infomation |
Other information: RET-IN-7 is a potent and selective small-molecule RET inhibitor with the CAS number 2763386-05-4. It is a valuable chemical probe for dissecting the biology of the RET signaling pathway in cancer and for developing targeted therapies. It is supplied as a solid and should be stored at -20degC.
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| Molecular Formula |
C22H24CLFN6O2
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|---|---|
| Molecular Weight |
458.916366577148
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| Exact Mass |
458.163
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| CAS # |
2763386-05-4
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| PubChem CID |
162641050
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
32
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| Complexity |
706
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N(C12CCC(N3C=C(C4C=C(N)C(Cl)=CC=4F)C4=C(N=CN=C34)N)(CC1)CC2)C(=O)OC
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| InChi Key |
FJTQBVRKZLEDPK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H24ClFN6O2/c1-32-20(31)29-21-2-5-22(6-3-21,7-4-21)30-10-13(17-18(26)27-11-28-19(17)30)12-8-16(25)14(23)9-15(12)24/h8-11H,2-7,25H2,1H3,(H,29,31)(H2,26,27,28)
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| Chemical Name |
methyl N-[4-[4-amino-5-(5-amino-4-chloro-2-fluorophenyl)pyrrolo[2,3-d]pyrimidin-7-yl]-1-bicyclo[2.2.2]octanyl]carbamate
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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: 16.67 mg/mL (36.32 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 | 2.1790 mL | 10.8951 mL | 21.7903 mL | |
| 5 mM | 0.4358 mL | 2.1790 mL | 4.3581 mL | |
| 10 mM | 0.2179 mL | 1.0895 mL | 2.1790 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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