SML2875

DCC-2618

≥98% (HPLC)

• Synonim(y): DCC 2618, DCC2618, N-(2,5-Difluoro-4-(2-(1-methyl-1H-pyrazol-4-yl)pyridin-4-yloxy)phenyl)-N′-phenylcyclopropane-1,1-dicarboxamide, c-Kit-IN-1
• Wzór empiryczny (zapis Hilla): C₂₆H₂₁F₂N₅O₃
• Numer CAS: 1225278-16-9
• Masa cząsteczkowa: 489.47
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD22571733
• Assay: ≥98% (HPLC)
• Form: powder

Właściwości

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: −20°C
• SMILES string: O=C(NC1=CC=CC=C1)C2(CC2)C(NC(C=C3F)=C(F)C=C3OC4=CC(C5=CN(C)N=C5)=NC=C4)=O
• InChI: 1S/C26H21F2N5O3/c1-33-15-16(14-30-33)21-11-18(7-10-29-21)36-23-13-19(27)22(12-20(23)28)32-25(35)26(8-9-26)24(34)31-17-5-3-2-4-6-17/h2-7,10-15H,8-9H2,1H3,(H,31,34)(H,32,35)
• InChI key: WWOXKWLDMLMYQY-UHFFFAOYSA-N

Opis

Biochem/physiol Actions

DCC-2618 is an orally active, potent type II switch pocket (SP) inhibitor against c-KIT (IC₅₀ = 4 nM/WT, 8 nM/V654A, 18 nM/T670I, 5 nM/D816H, 14 nM/D816V) and PDGFR. DCC-2618 locks c-KIT & PDGFR in an inactive conformation and is effective against multiple clinical forms of mutations resistant to type I ATP (catalytic)-site inhibitors Imatinib and Sunitinib. DCC-2618 inhibits cellular c-KIT activation (IC₅₀ = 36 nM/WT, 2 nM/ex 11 del, 7 nM/ex 11 del & V654A, 53 nM/V560D & D820A) and is efficacious against KIT mutants-mediated cancer growth in cultres (IC₅₀ = 2 nM; GIST with KIT D816Y) and in mice in vivo (50 mg/kg b.i.d. p.o.; GIST with KIT delW557K558/Y823D, AML with KIT N822K).

Orally active, potent type II switch pocket (SP) c-KIT & PDGFR inhibitor against multiple clinical forms of mutations resistant to Imatinib and Sunitinib.

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• Co się dzieje?: WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable