| Company Name: |
J & K SCIENTIFIC LTD.
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| Tel: |
010-82848833 400-666-7788 |
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jkinfo@jkchemical.com |
| Products Intro: |
Product Name:CUR 61414
CAS:334998-36-6
Package:10Mg,1Mg
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| | CUR 61414 Basic information |
| Product Name: | CUR 61414 | | Synonyms: | CUR 61414;N-[(3S,5S)-1-(1,3-Benzodioxol-5-ylmethyl)-5-(1-piperazinylcarbonyl)-3-pyrrolidinyl]-N-[(3-methoxyphenyl)methyl]-3,3-dimethylbutanamide;N-[(3S,5S)-1-(1,3-Benzodioxol-5-ylmethyl)-5-(1-piperazinylcarbonyl)-3-pyrrolidinyl]-N-[(3-methoxyphenyl)methyl]-3,3-dimethyl-benzamide;N-[(3S,5S)-1-(1,3-benzodioxol-5-ylmethyl)-5-(piperazine-1-carbonyl)pyrrolidin-3-yl]-N-[(3-methoxyphenyl)methyl]-3,3-dimethylbutanamide;Butanamide, N-[(3S,5S)-1-(1,3-benzodioxol-5-ylmethyl)-5-(1-piperazinylcarbonyl)-3-pyrrolidinyl]-N-[(3-methoxyphenyl)methyl]-3,3-dimethyl-;CUR61414,CUR-61414 | | CAS: | 334998-36-6 | | MF: | C31H42N4O5 | | MW: | 550.69 | | EINECS: | | | Product Categories: | All Inhibitors;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Bases & Related Reagents;Heterocycles;Nucleotides;Heterocycles, Inhibitors, Nucleotides, Bases & Related Reagents, Pharmaceuticals, Intermediates & Fine Chemicals | | Mol File: | 334998-36-6.mol |  |
| | CUR 61414 Chemical Properties |
| 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. |
| Hazard Codes | T | | Risk Statements | 25 | | Safety Statements | 45 | | RIDADR | UN 2811 6.1 / PGIII | | WGK Germany | 3 |
| | CUR 61414 Usage And Synthesis |
| Description | CUR 61414 is a potent inhibitor of hedgehog-induced cellular activity (IC50 = 100-200 nM). It binds directly with the pathway activator Smoothened (Ki = 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 |
| | CUR 61414 Preparation Products And Raw materials |
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