SML2875
DCC-2618
≥98% (HPLC)
别名:
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
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关于此项目
经验公式（希尔记法）:
C26H21F2N5O3
化学文摘社编号:
分子量:
489.47
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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)
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 key
WWOXKWLDMLMYQY-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
Quality Level
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Cancer discovery, 7(2), 121-122 (2017-01-13)
Tyrosine kinase inhibitors may initially control gastrointestinal stromal tumors, but most patients eventually experience disease progression due to activation loop mutations, which are resistant to approved drugs. However, phase I trials suggest that the cancer is sensitive to two new
Mathias Schneeweiss et al.
Haematologica, 103(5), 799-809 (2018-02-14)
Systemic mastocytosis is a complex disease defined by abnormal growth and accumulation of neoplastic mast cells in various organs. Most patients exhibit a D816V-mutated variant of KIT, which confers resistance against imatinib. Clinical problems in systemic mastocytosis arise from mediator-related
DCC-2618 is a potent inhibitor of wild-type and mutant KIT, including refractory Exon 17 D816 KIT mutations, and exhibits efficacy in refractory GIST and AML xenograft models, [abstract]
Smith BD, Hood MM, Wise SC, Kaufman MD, Lu WP, Rutkoski T, Flynn DL, Heinrich MC.
Cancer Research, 75 (15 Suppl), Abstract nr 2690-Abstract nr 2690 (2015)
DCC-2618, a pan KIT and PDGFR switch control inhibitor, achieves proof-of-concept in a first-in-human study
Janku F, George S, Razak A, Gordon M, Brooks D, Flynn DG, Kaufman M, Pitman J, Smith B, et al
European Journal of Cancer, 69, S4 (suppl-S4 (suppl (2016)
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