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Conteltinib (CT-707) is a novel and potent tyrosine kinase inhibitor with antineoplastic activitiy. It acts a multi-kinase inhibitor targeting FAK, ALK, and Pyk2.
| ln Vitro |
Conteltinib (CT-707) inhibits hepatocellular cancer by preventing FAK activation produced by XL184 in a synergistic manner [1]. In a human hepatocyte mitochondrial line, the combination of XL184 (5 μM) with Conteltinib (3 μM) led in heightened caspase-dependent cellular inflammation. This combination was much more efficacious than the solution medication alone [1]. Obesity rate is decreased and XL184 (5 μM) is induced by FAK phosphorylation [1].
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|---|---|
| ln Vivo |
HepG2 xenografts show good anti-tumor effects in nude mice when combined with CT-707 (ig 50 mg/kg twice daily for first 3 days, days 7, 8, 11, 12, and 14; once daily on days 4, 6, 9, 10, and 13; do not agree on day 5). XL184 (20 mg/kg once a day for the first 3 days; 10 mg/kg ig once a day on the 4th day; no dose on days 5 to 10; 10 mg/kg ig once a day on days 10 to 14).
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| Cell Assay |
Cell viability assay [1]
Cell Types: Human hepatoma cell lines HepG2 and Bel-7402 Tested Concentrations: 1.0, 1.5, 2.0, 2.5 and 3.0 μM for HepG2 cells; 0.2, 0.4, 0.8, 1.5 and 3.0 μM for Bel-7402 cells Incubation Duration: 72 hrs (hours) Experimental Results: When cells were exposed to XL184 (5 μM), Conteltinib (3 μM), or their combination, survival rates were 57.3% and 39.3% and 11.2% respectively in HepG2; 57.8% in Bel-7402 %, 61.6% and 34.2%. Apoptosis analysis [1] Cell Types: HepG2 and Bel-7402 Cell Tested Concentrations: 3 μM Incubation Duration: 48 hrs (hours) Experimental Results: The apoptosis rates of the control group, XL184, Conteltinib and combination groups in HepG2 were 5.0%, 10.5%, respectively. 18.4%, and 41.1%, and Bel-7402 was 4.4%, 16.3%, 8.7%, and 36.4%, respectively. Western Blot Analysis[1] Cell Types: HepG2 and Bel-7402 Tested Concentrations: 3 μM Incubation Duration: 24 hrs (hours) Experimental Results: XL184-induced FAK phosphorylation was Dramatically diminished, which may be part of the reason for the synergistic effect. |
| Animal Protocol |
Animal/Disease Models: Nude mice transplanted with HepG2 xenografts [1]
Doses: 50 mg/kg Route of Administration: intragastric (po) (po)(ig), twice a day for the first 3 days, days 7, 8, 11, Days 12 and 14; one time/day on days 4, 6, 9, 10, and 13; no administration on day 5. Experimental Results: Result in modest reduction in relative tumor volume (RTV). The inhibition rate of the combination group reached 77.4%, while the tumor weight of XL184 or CT-707 alone was suppressed by 30.7% and 19.4% respectively. |
| References |
| Molecular Formula |
C32H45N9O3S
|
|---|---|
| Molecular Weight |
635.823204755783
|
| Exact Mass |
635.336
|
| CAS # |
1384860-29-0
|
| PubChem CID |
89860551
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| Appearance |
Light yellow to yellow solid powder
|
| LogP |
5.1
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| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
45
|
| Complexity |
1030
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S(C1C=CC=CC=1NC1=C2C(=NC(=N1)NC1C=CC(=CC=1OC)N1CCC(CC1)N1CCN(C)CC1)NCC2)(NC(C)C)(=O)=O
|
| InChi Key |
NPJCURIANJMFEO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C32H45N9O3S/c1-22(2)38-45(42,43)29-8-6-5-7-27(29)34-31-25-11-14-33-30(25)36-32(37-31)35-26-10-9-24(21-28(26)44-4)40-15-12-23(13-16-40)41-19-17-39(3)18-20-41/h5-10,21-23,38H,11-20H2,1-4H3,(H3,33,34,35,36,37)
|
| Chemical Name |
2-[[2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-N-propan-2-ylbenzenesulfonamide
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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 : ~31.25 mg/mL (~49.15 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.27 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 20.8 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: ≥ 2.08 mg/mL (3.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5728 mL | 7.8639 mL | 15.7277 mL | |
| 5 mM | 0.3146 mL | 1.5728 mL | 3.1455 mL | |
| 10 mM | 0.1573 mL | 0.7864 mL | 1.5728 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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