CUR 61414 Property

Melting point:

35-40°C

Boiling point:

714.1±60.0 °C(Predicted)

Density 

1.24±0.1 g/cm3(Predicted)

storage temp. 

Hygroscopic, -20°C Freezer, Under Inert Atmosphere

solubility 

DMSO: soluble2mg/mL (clear solution, warmed)

pka

8.42±0.10(Predicted)

form 

powder

color 

white to beige

Stability:

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.

Safety

Hazard Codes 

T

Risk Statements 

25

Safety Statements 

45

RIDADR 

UN 2811 6.1 / PGIII

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

Precautionary statements

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

CUR 61414 Chemical Properties,Usage,Production

Description

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.

Chemical Properties

Pale Yellow Solid

Uses

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

References

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