| Identification | Back Directory | [Name]
Conteltinib
(CT-707) | [CAS]
1384860-29-0 | [Synonyms]
CT-707
Conteltinib
(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)- | [Molecular Formula]
C32H45N9O3S | [MDL Number]
MFCD32174265 | [MOL File]
1384860-29-0.mol | [Molecular Weight]
635.82 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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