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Vismodegib | Sonic Hedgehog signaling pathway inhibitor

A potent and selective Hedgehog (Hh) pathway signaling inhibitor antagonizing SMO with a Ki of 1.3 nM).1 Alters intracellular Ca2+ homeostasis and inhibits growth of cisplatin-resistant lung cancer cells.2  Inhibits two ABC transporters, ABCG2/BCRP and ABCB1/Pgp, IC50s=1.4 and 3.0 mM respectively.3 Clinically useful for the treatment of basal cell carcinoma.4 Inhibits proliferation and induces apoptosis in colon cancer cell lines.5
Induces apoptosis in pancreatic cancer stem cells6 and medulloblastoma7 and in basal-cell carcinoma stem cells8.

 

 

References/Citations
1) Rominger et al. (2009), Evidence for allosteric interactions of antagonist binding to the smoothened receptor; J. Pharmacol. Exp. Therap., 329 995
2) Tian et al. (2012), The hedgehog pathway inhibitor GDC-0449 alters intracellular Ca2+ homeostasis and inhibits cell growth in cisplatin-resistant lung cancer cells; Anticancer Res., 32 89
3) Zhang et al. (2009), Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp; Neoplasia, 11 96
4) Cirrone and Harris (2012), Vismodegib anf the hedgehog pathway: a new treatment for basal cell carcinoma; Clin. Ther., 34 2039
5) Wu et al. (2017), Smoothened antagonist GDC-0449 (Vismodegib) inhibits proliferation and triggers apoptosis in colon cancer cell lines; Exp. Ther. Med., 13 2529
6)Singh et al. (2011) Hedgehog signaling antagonist GDC-0449 (Vismodegib) inhibits pancreatic cancer stem cell characteristics: molecular mechanisms; PLoS One 6(11) e27306
7) Rudin et al. (2009) Treatment of medulloblastoma with hedgehog pathway inhibitor GDC-0449; N. Engl. J. Med., 361(12) 1173
8) Von Hoff et al. (2009) Inhibition of the hedgehog pathway in advanced basal-cell carcinoma; N. Engl. J. Med., 361(12) 1164

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Catalog#  10-2182

$60.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
879085-55-9
Catalog Number:
10-2182
Activity:
Sonic Hedgehog signaling pathway inhibitor
Chemical Name:
2-Chloro-N-(4-chloro-3-(pyridine-2-yl)phenyl)-4-(methylsulfonyl)benzamide
Alternate Names:
GDC-0449
Molecular Weight:
421.3
Molecular Formula:
C19H14Cl2N2O3S
Solubility:
Soluble in DMSO (up to 200 mg/ml) or in Ethanol (up to 10 mg/ml with warming)
Physical Properties:
Off-white or beige solid
Purity:
99% by TLC and HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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