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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
UNC1062 targets MERTK, a member of the TAM (TYRO3, AXL, MERTK) family of receptor tyrosine kinases. It exhibits specificity for MERTK, with IC50 values of 60 nM for TYRO3 and 85 nM for AXL. By inhibiting MERTK, it blocks downstream signaling pathways that promote tumor cell survival, proliferation, and invasion. Its high selectivity makes it a valuable tool for studying MERTK biology.
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| ln Vitro |
In vitro, UNC1062 reduces activation of MERTK-mediated downstream signaling, induces apoptosis in culture, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. Its inhibitory activity is typically assessed using kinase assays and cell-based functional assays. These studies confirm its potential as a therapeutic agent for MERTK-driven cancers.
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| ln Vivo |
In vivo activity of UNC1062 has been studied in animal models of cancer, including melanoma, gastric cancer, and acute myeloid leukemia. It has shown anti-tumor activity by inhibiting MERTK signaling. These studies provide evidence for its therapeutic potential in various malignancies.
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| Enzyme Assay |
Cell-free assays for UNC1062 typically involve measuring its inhibitory activity against MERTK using a biochemical kinase assay. The IC50 value of 1.1 nM and Ki of 0.33 nM are determined by measuring the phosphorylation of a peptide substrate in the presence of varying concentrations of the compound. These assays are used to characterize the compound's potency and selectivity.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of UNC1062. Melanoma and other cancer cell lines are treated with the compound, and cell proliferation, apoptosis, and invasion are measured. MERTK phosphorylation and downstream signaling are assessed to confirm target engagement. These assays confirm that UNC1062 effectively blocks MERTK-mediated cellular responses.
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| Animal Protocol |
In vivo animal experiments typically involve xenograft models of melanoma, gastric cancer, or acute myeloid leukemia. Animals are administered the compound via oral gavage or injection. Tumor growth is monitored over time to assess efficacy. Pharmacokinetic studies are conducted to measure plasma concentrations of the compound.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of UNC1062 are typical of a small molecule kinase inhibitor. Its molecular weight is 514.64. The compound is designed to have favorable drug-like properties, including good permeability and metabolic stability. Pharmacokinetic studies in animal models involve measuring plasma concentrations of the compound over time to determine its half-life, clearance, and volume of distribution.
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| Toxicity/Toxicokinetics |
The toxicity profile of UNC1062 is not extensively documented, but it is likely to be similar to other kinase inhibitors. Common adverse effects may include fatigue, diarrhea, and nausea. In preclinical studies, the compound has been shown to be well-tolerated at therapeutic doses, with a safety profile that supports its use in research.
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| References | |
| Additional Infomation |
UNC1062 is a research compound used to study MERTK and its role in cancer and immunology. It is a highly selective MERTK inhibitor. The compound is not approved for therapeutic use and is intended for research purposes only.
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| Molecular Formula |
C25H34N6O4S
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|---|---|
| Molecular Weight |
514.64
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| Exact Mass |
514.236
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| CAS # |
1350549-36-8
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| PubChem CID |
68212798
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
744.0±70.0 °C at 760 mmHg
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| Flash Point |
403.8±35.7 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.697
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| LogP |
2.66
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
36
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| Complexity |
791
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCNC1=NC=C2C(=NN(C2=N1)C3CCC(CC3)O)C4=CC=C(C=C4)S(=O)(=O)N5CCOCC5
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| InChi Key |
KAAPXWSYROPAEL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H34N6O4S/c1-2-3-12-26-25-27-17-22-23(29-31(24(22)28-25)19-6-8-20(32)9-7-19)18-4-10-21(11-5-18)36(33,34)30-13-15-35-16-14-30/h4-5,10-11,17,19-20,32H,2-3,6-9,12-16H2,1H3,(H,26,27,28)
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| Chemical Name |
4-[6-(butylamino)-3-(4-morpholin-4-ylsulfonylphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]cyclohexan-1-ol
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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: 10 mg/mL (19.43 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 | 1.9431 mL | 9.7155 mL | 19.4311 mL | |
| 5 mM | 0.3886 mL | 1.9431 mL | 3.8862 mL | |
| 10 mM | 0.1943 mL | 0.9716 mL | 1.9431 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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