Description
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.
Product information
CAS Number: 1384860-29-0
Molecular Weight: 635.82
Formula: C32H45N9O3S
Chemical Name: 2-{[2-({2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5H,6H,7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino}-N-(propan-2-yl)benzene-1-sulfonamide
Smiles: CN1CCN(CC1)C1CCN(CC1)C1=CC(OC)=C(C=C1)NC1N=C2NCCC2=C(NC2=CC=CC=C2S(=O)(=O)NC(C)C)N=1
InChiKey: NPJCURIANJMFEO-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 31.25 mg/mL (49.15 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Conteltinib (CT-707) synergizes with XL184 to suppress hepatocellular carcinoma by blocking XL184-induced FAK activation. The combination of XL184 (5 μM) and Conteltinib (3 μM) significantly reduces the survival fraction, compared with each agent alone. The combination of XL184 (5 μM) and Conteltinib (3 μM) results in enhanced caspase-dependent apoptosis in human hepatocellular carcinoma cell lines. The FAK phosphorylation induced by XL184 (5 μM) might be involved in the synergistic antitumor effect of Conteltinib (3 μM) and XL184.
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.
Products are for research use only. Not for human use.
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