Antibodies
AZD2461
- 貨號 Cat. No.
- S7029
- 規格 Size
- 10mM/1mL~25mg
- 品牌 Brand
- Selleckchem
Description
AZD2461
Catalog No.S7029
AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1. | |||||
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| Targets | ||||||
| IC50 | ||||||
| In vitro | AZD2461 has lower affinity for Pgp than does Olaparib. [1] | |||||
| In vivo | AZD2461 has an 80-fold increased Mdr1b expression on Olaparib-resistant KB1P tumor T6-28, without inhibition of Pgp. AZD2461 induces loss of 53BP1 expression in mice with KB1P tumors with short-term treatment. Long-term AZD2461 treatment is well tolerated and doubled the median relapse-free survival. [1] | |||||
| Features | ||||||
Protocol(Only for Reference)
Animal Study: [1]
| Animal Models | Olaparib-resistant tumors from KB1PM1, KB1PM3, and KB1PM4 in female mice |
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| Dosages | 100 mg/kg |
| Administration | p.o. |
| Solubility | 0.5% hyroxyethylcellulose/0.1% Tween 80 5 mg/mL |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01247168 | Completed | Refractory Solid Tumors|Cancer Tumor | AstraZeneca | 2010-11 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 395.43 |
|---|---|
| Formula | C22H22FN3O3 |
| CAS No. | 1174043-16-3 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 79 mg/mL (199 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 31 mg/mL (78 mM) | ||
| In vivo | 0.5% hyroxyethylcellulose/0.1% Tween 80 | 5 mg/mL | |
| * <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 | 1(2H)-Phthalazinone, 4-[[4-fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]- |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.39543 | 3.9543 | 7.9086 | 11.8629 |
