Altiratinib (DCC-2701) | MET/TIE-2/VEGFR inhibitor | Probechem Biochemicals

Chemical Structure : Altiratinib

CAS No.: 1345847-93-9

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Altiratinib (DCC-2701, DCC2701)

货号: PC-38624Not For Human Use, Lab Use Only.

Altiratinib (DCC-2701) is a potent c-MET/TIE-2/VEGFR inhibitor with IC50 of 2.7 nM (MET WT), 8.0 nM (TIE2 kinase) and 9.2 nM (VEGFR2), also potently inhibits oncogenic MET mutations in the switch region (residues 1228, 1230, and 1250) with IC50 range of 0.37-6 nM.

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25 mg	￥1480	In stock
50 mg	￥2280	In stock
100 mg	￥3880	In stock
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生物&药学活性

Altiratinib (DCC-2701) is a potent c-MET/TIE-2/VEGFR inhibitor with IC50 of 2.7 nM (MET WT), 8.0 nM (TIE2 kinase) and 9.2 nM (VEGFR2), also potently inhibits oncogenic MET mutations in the switch region (residues 1228, 1230, and 1250) with IC50 range of 0.37-6 nM.
Altiratinib (DCC-2701) also potently inhibited TRKA, TRKB, and TRKC (NTRK3) kinases with IC50 values of 0.85 nM, 4.6 nM, and 0.83 nM, respectively.
Altiratinib (DCC-2701) is >10-fold selective for MET versus FMS and KIT, and >50-fold selective for MET versus ABL1, FYN, HER1 (EGFR), p38a (MAPK14), PDGFRa, PDGFRb, RET, and SRC.
Altiratinib (DCC-2701) inhibited HGF-stimulated MET phosphorylation in HUVECs, exhibiting an IC50 of 2.3 nM, inhibited VEGFR2 phosphorylation with an IC50 of 4.7 nM in VEGF-stimulated HUVECs.
Altiratinib (DCC-2701) exhibits robust pharmacology in tumor models driven by genomic MET mutation as well as in models of microenvironment activation of MET.

物理化学性质&存储条件

分子量	510.47
分子式	C26H21F3N4O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-[4-[[2-[(Cyclopropylcarbonyl)amino]-4-pyridinyl]oxy]-2,5-difluorophenyl]-N′-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide

参考文献

1. Smith BD, et al. Mol Cancer Ther. 2015 Sep;14(9):2023-34.

2. Kwon Y, et al. Oncogene. 2015 Jan 8;34(2):144-53.

Altiratinib (DCC-2701, DCC2701)

生物&药学活性

物理化学性质&存储条件

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Altiratinib (DCC-2701, DCC2701)

生物&药学活性

物理化学性质&存储条件

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