CUR 61414 Struktur

CUR 61414

Bezeichnung:CUR 61414

CAS-Nr334998-36-6

Englisch Name:CUR 61414

CBNumberCB31565488

SummenformelC31H42N4O5

Molgewicht550.69

MOL-Datei334998-36-6.mol

CUR 61414 physikalisch-chemischer Eigenschaften

Schmelzpunkt	35-40°C
Siedepunkt	714.1±60.0 °C(Predicted)
Dichte	1.24±0.1 g/cm3(Predicted)
storage temp.	Hygroscopic, -20°C Freezer, Under Inert Atmosphere
Löslichkeit	DMSO: soluble2mg/mL (clear solution, warmed)
pka	8.42±0.10(Predicted)
Aggregatzustand	powder
Farbe	white to beige
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25
S-Sätze:	45
RIDADR	UN 2811 6.1 / PGIII
WGK Germany	3

Gefahreninformationscode (GHS)

CUR 61414 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
CUR 61414 is a potent inhibitor of hedgehog-induced cellular activity (IC₅₀ = 100-200 nM). It binds directly with the pathway activator Smoothened (K_i = 44 nM). CUR 61414 blocks proliferation and induces apoptosis in mouse basal cell carcinoma and causes regression of basaloid lesions triggered by ultraviolet light in mouse skin.
Chemische Eigenschaften
Pale Yellow Solid
Verwenden
CUR 61414 is a proline derivative as mediator of hedgehog signaling pathways for pharmaceutical and cosmetic uses. CUR 61414 is a Nucleoside analog. CUR 61414 is an antimetabolite antitumor combination Gemcitabine cancer treatment
in vitro
previous study found that cur61414 was able to arrest proliferation of basal cells within the bcc-like lesions and induce cells to undergo apoptosis resulting in complete regression of the lesions, without affecting neighboring skin cells [1].
in vivo
the efficacy of cur61414 against basaloid lesions induced when mice were exposed to uv light. these mice were uv irradiated for 6-9 months, producing many microscopic bcc-like basaloid lesions throughout their skin. results showed that the treatment with cur61414 could cause regression of these lesions, as demonstrated by both x-gal staining and histological analyses. moreover, the regression in the cur61414-treated mice seemed to be the result of massive cell death, becuase a significant increase in apoptotic nuclei was seen in basaloid nests after treatment. in addition, no overt toxicity was observed in the skin surrounding the lesions [1].
IC 50
100-200 nm for hedgehog-induced cellular activity
Einzelnachweise
1) Williams et al. (2003), Identification of a small molecule inhibitor of the hedgehog signaling pathway: effects on basal cell carcinoma-like lesions; Proc.Natl. Acad. Sci. USA, 100 4616 2) Tang et al. (2011), Targeting superficial or nodular Basal cell carcinoma with topically formulated small molecule inhibitor of smoothened; Clin. Cancer Res., 17 3378 3) Athar et al. (2004), Inhibition of smoothened signaling prevents ultraviolet B-induced basal cell carcinomas through regulation of Fas expression and apoptosis; Sci. Signal., 64 7545

CUR 61414 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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