Antibodies
R428 (BGB324)
- 貨號 Cat. No.
- S2841
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
R428 (BGB324)
Catalog No.S2841
R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).
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Biological Activity
| Description | R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective). | |||||
|---|---|---|---|---|---|---|
| Targets | Axl | |||||
| IC50 | 14 nM [1] | |||||
| In vitro | R428 blocks the catalytic and procancerous activities of Axl. R428 inhibits Axl with low nanomolar activity and blocks Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production. [1] In a recent study, the Axl inhibitor R428 shows a mean IC50 dose of ∼ 2.0μM for the primary CLL B cells after 24 hours of treatment and normal B-, T-, and natural killer (NK) cells show no significant amount of cell death at this dose of R428 (2.5 μM) under similar experimental conditions. [2] | |||||
| In vivo | Pharmacologic investigations reveal favorable exposure after oral administration such that R428-treated tumors display a dose-dependent reduction in expression of the cytokine granulocyte macrophage colony-stimulating factor and the epithelial-mesenchymal transition transcriptional regulator Snail. In support of an earlier study, R428 inhibits angiogenesis in corneal micropocket and tumor models. R428 administration reduces metastatic burden and extends survival in MDA-MB-231 intracardiac and 4T1 orthotopic (median survival, >80 days compared with 52 days; P < 0.05) mouse models of breast cancer metastasis. [1] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| In vitro Kinase Assays | A five-point R428 dose titration is performed in radiometric in vitro kinase assays on 133 kinases at the KmATP for each kinase. Axl, Mer, and Tyro3 assays are also performed using a fluorescence polarization protocol. HER2 activity is determined by Z’-LYTE assay. |
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Animal Study: [1]
| Animal Models | MDA-MB-231-luc-D3H2LN Intracardiac Model |
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| Dosages | 125 mg/kg |
| Administration | Oral, twice daily |
| Solubility | 0.5% hyroxyethylcellulose/0.1% Tween 80, 7 mg/mL |
References
Chemical Information
| Molecular Weight (MW) | 506.64 |
|---|---|
| Formula | C30H34N8 |
| CAS No. | 1037624-75-1 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 60 mg/mL (118 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 0.5% hyroxyethylcellulose/0.1% Tween 80, | 7 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 | 1H-1,2,4-Triazole-3,5-diamine, 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5H-benzocyclohepten-2-yl]- |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.50664 | 5.0664 | 10.1328 | 15.1992 |
