| Identification | Back Directory | [Name]
DCC-2618 | [CAS]
1225278-16-9 | [Synonyms]
CS-937
DCC-2618
c-Kit-IN-1
DCC-2618, >98%
DCC-2618?, >98%
DCC2618;DCC 2618
c-Kit inhibitor 1
PDGFR inhibitor 1
DCC-2618 USP/EP/BP
c-Kit-IN-1(DCC-2618)
PDGFR inhibitor 1, DCC-2618
N-[2,5-Difluoro-4-[[2-(1-methyl-1H-pyrazol-4-yl)-4-pyridinyl]oxy]phenyl]-N'-phenyl-1,1-cyclopropanedicarboxamide
1,1-Cyclopropanedicarboxamide, N-[2,5-difluoro-4-[[2-(1-methyl-1H-pyrazol-4-yl)-4-pyridinyl]oxy]phenyl]-N'-phenyl-
N-[2,5-Difluoro-4-[[2-(1-methyl-1H-pyrazol-4-yl)-4-pyridinyl]oxy]phenyl]-N'-phenyl-1,1-cyclopropanedicarboxamide DCC-2618 | [Molecular Formula]
C26H21F2N5O3 | [MDL Number]
MFCD22571733 | [MOL File]
1225278-16-9.mol | [Molecular Weight]
489.47 |
| Chemical Properties | Back Directory | [Boiling point ]
729.7±60.0 °C(Predicted) | [density ]
1.40±0.1 g/cm3 (20 ºC 760 Torr) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 20 mg/ml; DMF:PBS (pH 7.2) (1:5): 0.1 mg/ml; DMSO: 14 mg/ml; Ethanol: Partially soluble | [form ]
Powder | [pka]
12.10±0.70(Predicted) | [color ]
White to off-white | [InChIKey]
WWOXKWLDMLMYQY-UHFFFAOYSA-N | [SMILES]
C1(C(NC2=CC=CC=C2)=O)(C(NC2=CC(F)=C(OC3C=CN=C(C4=CN(C)N=C4)C=3)C=C2F)=O)CC1 |
| Hazard Information | Back Directory | [Uses]
c-Kit-IN-1 is a potent inhibitor of c-Kit and c-Met with IC50s of <200 nM. | [Biological Activity]
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). | [target]
wt c-KIT | [References]
[1] Daniel L. Flynn, et al. Cyclopropane amides and analogs exhibiting anti-cancer and anti-proliferative activities. WO 2010051373 A1 |
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| Company Name: |
Twochem Co.Ltd. Gold
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
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