Antibodies
HER2-Inhibitor-1
- 貨號 Cat. No.
- S2752
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
HER2-Inhibitor-1
ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR. Phase 1.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR. Phase 1. | |||||
|---|---|---|---|---|---|---|
| Targets | HER2 | |||||
| IC50 | 8 nM [1] | |||||
| In vitro | ARRY-380 is equipotent against truncated p95-HER2 with IC50 of 7 nM. [1] However, ARRY-380 suppresses EGFR with IC50 of 4 μM. ARRY-380 is about 500-fold selective for HER2 versus EGFR. [1] | |||||
| In vivo | ARRY-380 significantly prevents the growth of tumor in multiple HER2-dependent tumor xenograft models and displays additive activity in combination with standard-of-care agents. [1] | |||||
| Features | ||||||
Protocol(Only for Reference)
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00650572 | Completed | Cancer | Array BioPharma | 2008-05 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 569.63 |
|---|---|
| Formula | C29H27N7O4S |
| CAS No. | 937265-83-3 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 114 mg/mL (200 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 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 | N-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-amine |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.56963 | 5.6963 | 11.3926 | 17.0889 |
Customer Reviews (1)
 Click to enlarge | Rating | |
| Source | HER2-Inhibitor-1 purchased from Selleck | |
| Method | Western Blotting | |
| Cell Lines | A431 cells | |
| Concentrations | 10 nM | |
| Incubation Time | 30 mins | |
| Results | Conclusion-P-EGFR (Tyr845) signal is inhibited in varying degree with EGF stimulation, and is not detectable without EGF stimulation. Inhibition results in table below right. |
