Antibodies
LY2940680
- 貨號 Cat. No.
- S2157
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
LY2940680
Catalog No.S2157
LY2940680 binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | LY2940680 binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2. | |||||
|---|---|---|---|---|---|---|
| Targets | Smo | |||||
| IC50 | ||||||
| In vitro | LY2940680 inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib. [1] | |||||
| In vivo | LY2940680 has excellent pharmacokinetic properties in rodent and non-rodent species. LY2940680 administrated orally treats Ptch+/- p53-/- transgenic mice which spontaneously develop medulloblastoma, produces remarkable efficacy and significantly improves their survival. LY2940680 reveals rapid kinetics of anti-tumor activity through magnetic resonance imaging of these mice, and LY2940680 induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. LY2940680 inhibits Hh regulated gene expression in the subcutaneous xenograft tumor stroma and produces significant anti-tumor activity. [2] | |||||
| Features | ||||||
Protocol(Only for Reference)
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01226485 | Recruiting | Advanced Cancer | Eli Lilly and Company | 2010-09 | Phase 1 |
| NCT01681186 | Completed | Healthy Volunteers | Eli Lilly and Company | 2012-09 | Phase 1 |
| NCT01722292 | Recruiting | Small Cell Lung Carcinoma | Eli Lilly and Company | 2013-01 | Phase 1|Phase 2 |
| NCT01746745 | Completed | Healthy Volunteers | Eli Lilly and Company | 2013-01 | Phase 1 |
| NCT01697514 | Not yet recruiting | Medulloblastoma, Childhood|Rhabdomyosarcoma | Eli Lilly and Company | 2013-07 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 512.5 |
|---|---|
| Formula | C26H24F4N6O |
| CAS No. | 1258861-20-9 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 0.66 mg/mL (1 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 2 mg/mL (3 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 4-fluoro-N-methyl-N-(1-(4-(1-methyl-1H-pyrazol-5-yl)phthalazin-1-yl)piperidin-4-yl)-2-(trifluoromethyl)benzamide |
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