R428 (BGB324)

R428 (BGB324)は一種のAxl阻害剤で、IC50値が14 nMです。R428 (BGB324)は、Axlに作用する選択性はAblに作用する選択性より100倍以上が高くなって、MerとTyro3に作用する選択性より50倍-100倍が高くなって、InsR、EGFR、HER2とPDGFRβに作用する選択性より100倍余りが高くなります。

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R428 (BGB324) 化学構造
分子量: 506.64





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製品説明 R428 (BGB324)は一種のAxl阻害剤で、IC50値が14 nMです。R428 (BGB324)は、Axlに作用する選択性はAblに作用する選択性より100倍以上が高くなって、MerとTyro3に作用する選択性より50倍-100倍が高くなって、InsR、EGFR、HER2とPDGFRβに作用する選択性より100倍余りが高くなります。
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 3年-20℃
2年-80℃in solvent
溶解度 (25°C) * In vitro DMSO 6 mg/mL warming (11.84 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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]-

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Frequently Asked Questions

  • Question 1
    Could you please let me know whether this compound is an enantiomer or it is in its racemic form?

    Answer: Our S2841 R428 is S enantiomer, and its e.e. value (enantiomeric purity) >98%.



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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID