| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
PDGFR; Bcr-Abl
INVIVO74978 targets multiple protein kinases, including those involved in the PDGF-R, c-Kit, and Bcr-abl pathways. These kinases are key drivers of cell proliferation and survival, and their aberrant activity is implicated in various cancers. By inhibiting these targets, INVIVO74978 can modulate multiple signaling pathways simultaneously, which is a common strategy for overcoming resistance and achieving robust antitumor effects. |
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| ln Vitro |
Multi-kinase inhibitor 1 (compound 68) is a potent multi-kinase inhibitor. The protein kinases are a large family of proteins that are essential for maintaining control over cellular function and for regulating a wide range of cellular processes. These kinases comprise non-receptor tyrosine kinases like the fusion kinase Bcr-abl as well as receptor tyrosine kinases like the receptor kinase for stem cell factor, c-Kit, and platelet derived growth factor receptor kinase (PDGF-R)[1].
In vitro, INVIVO74978 is characterized by its multi-kinase inhibitory activity. While specific IC50 values are not provided in the sources, its potency against targets like PDGF-R, c-Kit, and Bcr-abl is implied by its description as a potent inhibitor. Its activity is assessed in cell-based assays measuring the proliferation of kinase-dependent cancer cell lines or in biochemical assays measuring the activity of the purified kinases. |
| ln Vivo |
In vivo, INVIVO74978 is used in research to study the effects of multi-kinase inhibition. Its mechanism of targeting key oncogenic kinases makes it a candidate for study in animal models of cancer. By inhibiting PDGF-R, c-Kit, and Bcr-abl, it could potentially suppress tumor growth and overcome resistance to single-target therapies.
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| Enzyme Assay |
In vitro enzyme/receptor binding studies for INVIVO74978 are performed using kinase activity assays. In these assays, the target kinase (e.g., PDGF-R, c-Kit, Bcr-abl) is incubated with its substrate and ATP in the presence of varying concentrations of the inhibitor. The enzyme's activity is measured by detecting the phosphorylation of the substrate. The IC50 or Kd values are determined from these experiments, confirming the compound's inhibition of these kinases.
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| Cell Assay |
In vitro cellular assays for INVIVO74978 are used to study its effects on cancer cells. Cells that are dependent on the activity of its target kinases are treated with the compound. Key readouts include cell viability (MTT or CellTiter-Glo assays), apoptosis (Annexin V/PI staining), and the phosphorylation status of downstream targets of the inhibited kinases. These assays are crucial for confirming its mechanism of action and its potential as an anticancer agent.
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| Animal Protocol |
In vivo animal studies for INVIVO74978 are not extensively documented in the provided sources. As a multi-kinase inhibitor, it would be studied in xenograft models using cancer cell lines that are sensitive to the inhibition of its targets. Tumor-bearing mice would be treated with the compound, and endpoints would include tumor growth inhibition, survival, and pharmacodynamic analysis of target inhibition in the tumor tissue.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of INVIVO74978 are indicated by its molecular weight (not specified in the provided snippets) and its appearance as an off-white to yellow solid powder. Its density is 1.4 ± 0.1 g/cm³. Its solubility and other PK parameters are not detailed in the provided sources. For storage, it is typically kept at -20°C to maintain stability. These properties are important for its formulation and use in laboratory studies.
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| Toxicity/Toxicokinetics |
Toxicological data for INVIVO74978 are limited, as it is a research compound. Its primary value is as a tool for studying kinase signaling. While specific toxicity profiles are not detailed, its mechanism of inhibiting multiple kinases could potentially affect normal cellular processes. Comprehensive safety studies are not available in the public domain.
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| References | |
| Additional Infomation |
INVIVO74978 is a research-use-only compound that acts as a potent multi-kinase inhibitor. Its CAS number is 778274-97-8. It is also known as Multi-kinase inhibitor 1. This compound is a valuable tool for researchers studying the role of kinases in cancer and other diseases characterized by abnormal tyrosine kinase activity. It is not an approved drug.
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| Molecular Formula |
C20H17F3N4O3
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|---|---|
| Molecular Weight |
418.3762
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| Exact Mass |
418.125
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| Elemental Analysis |
C, 57.42; H, 4.10; F, 13.62; N, 13.39; O, 11.47
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| CAS # |
778274-97-8
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| Related CAS # |
778274-97-8
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| PubChem CID |
59983028
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
615.9±55.0 °C at 760 mmHg
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| Flash Point |
326.3±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.600
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
536
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(OC1C=CC(=CC=1)NC1=CC(C2C=CC(C(NCCO)=O)=CC=2)=NC=N1)(F)F
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| InChi Key |
DEGDCVFNFAOIPU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H17F3N4O3/c21-20(22,23)30-16-7-5-15(6-8-16)27-18-11-17(25-12-26-18)13-1-3-14(4-2-13)19(29)24-9-10-28/h1-8,11-12,28H,9-10H2,(H,24,29)(H,25,26,27)
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| Chemical Name |
N-(2-hydroxyethyl)-4-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide
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| Synonyms |
INVIVO 74978; Multi-kinase inhibitor I; INVIVO-74978; INVIVO74978
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: ~50 mg/mL (~100.2 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3902 mL | 11.9509 mL | 23.9017 mL | |
| 5 mM | 0.4780 mL | 2.3902 mL | 4.7803 mL | |
| 10 mM | 0.2390 mL | 1.1951 mL | 2.3902 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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