Conteltinib (CT-707)
Conteltinib (CT-707) Basic information
- Product Name:
- Conteltinib (CT-707)
- Synonyms:
-
- Conteltinib (CT-707)
- CT-707
- Benzenesulfonamide, 2-[[6,7-dihydro-2-[[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-N-(1-methylethyl)-
- N-Isopropyl-2-[[2-[[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidyl]phenyl]amino]-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]benzenesulfonamide
- N-Isopropyl-2-((2-((2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)benzenesulfonamide , Conteltinib
- N-Isopropyl-2-((2-((2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)benzenesulfonamide
- Conteltinib, 10 mM in DMSO
- CAS:
- 1384860-29-0
- MF:
- C32H45N9O3S
- MW:
- 635.82
- Mol File:
- 1384860-29-0.mol
Conteltinib (CT-707) Chemical Properties
- Boiling point:
- 814.7±75.0 °C(Predicted)
- Density
- 1.283±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 31.25 mg/mL (49.15 mM)
- form
- Solid
- pka
- 11.74±0.50(Predicted)
- color
- Light yellow to yellow
Conteltinib (CT-707) Usage And Synthesis
Uses
Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK, ALK, and Pyk2. Conteltinib exerts significant inhibitory effect on FAK with an IC50 of 1.6 nM[1].
in vivo
The combination of XL184 (20 mg/kg once daily for first 3 days; i.g. 10 mg/kg once a day for 4th day; no administration from 5th to 10th days; i.g. 10 mg/kg once a day from the 10th to 14th days )and CT-707 (i.g. 50 mg/kg twice a day for first 3 days, 7th, 8th, 11th, 12th, and 14th days; once a day for 4th, 6th, 9th, 10th, and 13th days; no administration for the 5th day) shows the synergistic antitumor effect in HepG2 xenograft nude mice[1].
| Animal Model: | Nude mice transplanted with HepG2 xenografts[1] |
| Dosage: | 50 mg/kg |
| Administration: | Intragastrically (i.g.) twice a day for first 3 days, 7th, 8th, 11th, 12th, and 14th days; once a day for 4th, 6th, 9th, 10th, and 13th days; no administration for the 5th day. |
| Result: | Caused a moderate decrease in the relative tumor volume (RTV). The inhibition rate of combination group reached 77.4%, whereas the mono-treatment of XL184 or CT-707 alone caused 30.7% and 19.4% inhibition in the tumor weight, respectively. |
References
[1] Wang DD, et al. CT-707, a Novel FAK Inhibitor, Synergizes with XL184 to Suppress Hepatocellular Carcinoma by Blocking XL184-Induced FAK Activation. Mol Cancer Ther. 2016 Dec;15(12):2916-2925. DOI:10.1158/1535-7163.MCT-16-0282
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