| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
UNC0064-12 targets VEGFR2 (vascular endothelial growth factor receptor 2), a receptor tyrosine kinase that plays a critical role in angiogenesis and tumor growth. VEGFR2 is the primary mediator of VEGF-induced endothelial cell proliferation, migration, and survival. By inhibiting VEGFR2, UNC0064-12 disrupts VEGF signaling and angiogenesis. The compound is a multi-kinase inhibitor, meaning it also inhibits other kinases in addition to VEGFR2. Its multi-target profile makes it useful for proteomics-based kinome analyses.
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| ln Vitro |
In vitro, UNC0064-12 is a VEGFR2 inhibitor and multi-kinase inhibitor. The compound has been used as an affinity ligand for proteomics-based kinome analyses of cancer cells. Its ability to inhibit VEGFR2 and other kinases has been characterized in kinase activity assays. However, specific IC50 values for VEGFR2 inhibition are not available in the provided literature. The compound's multi-kinase activity makes it useful for studying kinase signaling networks in cancer cells.
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| ln Vivo |
In vivo, UNC0064-12 has potential applications in studying angiogenesis and tumor growth due to its VEGFR2 inhibitory activity. However, detailed in vivo efficacy data are limited. The compound is primarily used as a research tool for in vitro and proteomics studies.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for UNC0064-12 involve measuring its inhibitory activity against VEGFR2 and other kinases using purified recombinant kinases. Kinase activity assays are performed with a peptide substrate and ATP in the presence of varying concentrations of UNC0064-12. Kinase activity is measured by quantifying phosphorylation of the substrate, and IC50 values are calculated from inhibition curves. The compound's multi-kinase profile is assessed by screening against a panel of kinases.
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| Cell Assay |
In vitro cell-based experiments for UNC0064-12 are conducted using cancer cell lines or endothelial cells. Cells are treated with UNC0064-12 at varying concentrations, and cell proliferation, migration, and tube formation (for endothelial cells) are assessed to evaluate VEGFR2 inhibition and anti-angiogenic activity. Signaling pathways (e.g., VEGFR2 phosphorylation, downstream MAPK and PI3K/AKT signaling) are assessed by Western blot.
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| Animal Protocol |
In vivo animal experiments for UNC0064-12 are performed in xenograft mouse models of cancer or in models of angiogenesis. The compound is administered, and tumor growth, angiogenesis, and vascular permeability are assessed. However, detailed in vivo efficacy data are limited.
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| ADME/Pharmacokinetics |
UNC0064-12 is a small molecule (MW 364.45, formula C19H24N8) with suitable physicochemical properties for research use. The compound is soluble in DMSO (10 mM). Its -NH2 terminal linker enables further synthesis and conjugation. Detailed pharmacokinetic parameters are limited in available literature.
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| Toxicity/Toxicokinetics |
Preclinical toxicology data for UNC0064-12 are limited. The compound is supplied for laboratory research use only and is not for human or veterinary use. As a multi-kinase inhibitor, potential off-target effects should be considered.
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| References | |
| Additional Infomation |
UNC0064-12 is also known as VEGFR-2-IN-5. It is a research compound used primarily as an affinity ligand for proteomics-based kinome analyses of cancer cells and for studying VEGFR2 signaling and angiogenesis. The compound is extracted from patent WO2013055780A1 and is not approved for clinical use.
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| Molecular Formula |
C19H24N8
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|---|---|
| Molecular Weight |
364.447462081909
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| Exact Mass |
364.212
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| Elemental Analysis |
C, 62.62; H, 6.64; N, 30.75
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| CAS # |
1430089-64-7
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| Related CAS # |
VEGFR-2-IN-5 hydrochloride;2700435-52-3
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| PubChem CID |
90369695
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| Appearance |
White to gray solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
693.5±65.0 °C at 760 mmHg
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| Flash Point |
373.2±34.3 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.757
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| LogP |
0.92
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
27
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| Complexity |
437
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NCCCNC1=CC=C(NC2=NC=CC(NC3=NNC(C4CC4)=C3)=N2)C=C1
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| InChi Key |
UYYZTTPXKIYERF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H24N8/c20-9-1-10-21-14-4-6-15(7-5-14)23-19-22-11-8-17(25-19)24-18-12-16(26-27-18)13-2-3-13/h4-8,11-13,21H,1-3,9-10,20H2,(H3,22,23,24,25,26,27)
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| Chemical Name |
2-N-[4-(3-aminopropylamino)phenyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
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| Synonyms |
UNC0064-12; UNC-0064-12; UNC006412; UNC 006412; UNC-006412; UNC 0064-12
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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 : ≥ 46 mg/mL (~126.22 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 | 2.7439 mL | 13.7193 mL | 27.4386 mL | |
| 5 mM | 0.5488 mL | 2.7439 mL | 5.4877 mL | |
| 10 mM | 0.2744 mL | 1.3719 mL | 2.7439 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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