R428 (BGB324) 化学構造
分子量: 506.64



Quality Control & MSDS


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製品説明 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).
ターゲット Axl
IC50 14 nM [1]
In vitro試験 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試験 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]

プロトコル (参考用のみ)

キナーゼアッセイ: [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.

動物実験: [1]

動物モデル MDA-MB-231-luc-D3H2LN Intracardiac Model
製剤 0.5% hydroxypropylmethylcellulose + 0.1% Tween 80
投薬量 125 mg/kg
投与方法 Oral, twice daily

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download R428 (BGB324) SDF
分子量 506.64


CAS No. 1037624-75-1
保管 2年-20℃
6月-80℃in solvent
溶解度 (25°C) * In vitro DMSO 24 mg/mL warmed (47.37 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 5% DMSO+corn oil 1mg/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.
化学名 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]-

カスタマーフィードバック (2)

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Source Cancer Res, 2014, 74(18), 5152-64. R428 (BGB324) purchased from Selleck
Method Western blot
Cell Lines HP cells
Concentrations 0-1.0 uM
Incubation Time 24 h
Results The small-molecule TKI R428, which has greater than 100-fold selectivity for AXL as compared with EGFR or Tyro and 50-fold greater affinity than Mer. R428 treatment led to a loss of EGFR phosphorylation on tyrosine 1068 and MAPK signaling, whereas these targets were relatively unaffected in HP cells.

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Source Biochem Bioph Res Co, 2014, 10.1016/j.bbrc.2014.10.126. R428 (BGB324) purchased from Selleck
Method Western blot, Annexin V
Cell Lines NB1643 cells
Concentrations 300 nM
Incubation Time 48 h
Results To further explore the application of Axl-specific small-molecule inhibitor in ALK-targeted therapy, we treated cells with BGB324 (an Axl inhibitor) in the presence of crizotinib (A)or ceritinib (B) and the frequency of apoptosis was measured by Annexin V binding assay. phosphorylated Axl and ALK were effectively suppressed by BGB324 and crizotinib respectively in NB1643 cells(C). Notably, combination treatment resulted in marked inhibition of the activities of Axl and ALK, as well as more efficiency in induction of activated-caspase3 than either single-drug alone, consistent with the increased apoptosis observed in the annexin V binding assay (A). Similar results were observed in the SHSY5Y cell lines (D), with combination treatment showing marked inhibition of phosphorylated Axl and ALK, as well as increased caspase3 cleavage.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID