5.31091
Porcn Inhibitor IV, LGK974
동의어(들):
Porcn Inhibitor IV, LGK974, 2-(2ʹ,3-Dimethyl-2,4ʹ-bipyridin-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide, Wnt Pathway Inhibitor XXIII, LGK-974
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크기 선택
제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C23H20N6O
CAS 번호:
Molecular Weight:
396.44
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
SMILES string
N(c3ncc(cc3)c4nccnc4)C(=O)Cc1cnc(c(c1)C)c2cc(ncc2)C
InChI
1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30)
InChI key
XXYGTCZJJLTAGH-UHFFFAOYSA-N
assay
≥97% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
tan
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Porcupine
Porcupine
Reversible: yes
Disclaimer
Toxicity: Standard Handling (A)
General description
A cell-permeable C59 (Cat. No. 500496) structural analog that potently inhibits Wnt secretion from L-cell Wnt1/2/3/3a/6/7a/9a transfectants (IC50 from 50 pM to 1.1 nM) via direct porcupine (Porcn), but not Wntless, affinity interaction. Shown to inhibit the proliferation of head and neck squamous cell carcinoma (HNSCC) line HN30 (IC50 = 0.3 nM), but not 293T even at a high concentration of 20 µM. In mice & rats receiving therapeutic LGK974 oral dosages (up to 5 mg/10 mL/kg/d), a delayed tissue Wnt signaling suppression (max inhibition 7 to 10 h post dosing) is seen due to pre-existing Wnt in tissue, followed by a full recovery of tissue Wnt signalling at 24 h upon drug clearance. The periodic daily inhibition/recovering cycle is shown to result in tumor regression in mice & rats, while allowing Wnt signaling-dependent normal tissue homeostasis. Overdosing is reported to result in loss of intestinal epithelium in rats receiving 14 consecutive 20 mg/kg daily oral dosages.
Other Notes
Liu, J., et al. 2013. Proc. Natl. Acad. Sci. USA110, 20224.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
시험 성적서(COA)
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