Zanubrutinib (BGB-3111)

製品コードS8791 バッチS879104

化学情報

	Synonyms	BGB-3111	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₇H₂₉N₅O₃
	分子量	471.55	CAS No.	1691249-45-2
Solubility (25°C)*	体外	DMSO	94 mg/mL (199.34 mM)
		Ethanol	94 mg/mL (199.34 mM)
		Water	Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Zanubrutinibは、ITK、JAK3、EGFRを含む他のキナーゼに対するオフターゲット阻害活性が低いことが示されている、強力で特異的かつ不可逆的なBTK阻害剤です。
in vitro	In biochemical and cellular assays, BGB-3111 is more selective than ibrutinib for BTK vs. EGFR, FGR, FRK, HER2, HER4, ITK, JAK3, LCK, BLK and TEC. In several MCL and DLBCL cell lines, BGB-3111 inhibits BCR aggregation-triggered BTK autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation.
in vivo	In preclinical animal studies, BGB-3111 demonstrates superior oral bioavailability, achieving higher exposure and more complete target inhibition in the tissues than ibrutinib. In mouse BTK occupancy assays, treatment with BGB-3111 results in a dose-dependent BTK occupancy and shows about 3-fold more potency than ibrutinib in target organs, including PBMC and spleen. Both in the REC-1 MCL and ABC subtype DLBCL (TMD-8) xenograft models, BGB-3111 induces dose-dependent anti-tumor effects and demonstrates superior efficacy in comparison with ibrutinib. Toxicity study in rats indicates that BGB-3111 is very well tolerated, and the MTD is not reached when it is dosed up to 250 mg/kg/day.

製品説明

Zanubrutinibは、ITK、JAK3、EGFRを含む他のキナーゼに対するオフターゲット阻害活性が低いことが示されている、強力で特異的かつ不可逆的なBTK阻害剤です。

in vitro

In biochemical and cellular assays, BGB-3111 is more selective than ibrutinib for BTK vs. EGFR, FGR, FRK, HER2, HER4, ITK, JAK3, LCK, BLK and TEC.

In several MCL and DLBCL cell lines, BGB-3111 inhibits BCR aggregation-triggered BTK autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation.

in vivo

In preclinical animal studies, BGB-3111 demonstrates superior oral bioavailability, achieving higher exposure and more complete target inhibition in the tissues than ibrutinib.

In mouse BTK occupancy assays, treatment with BGB-3111 results in a dose-dependent BTK occupancy and shows about 3-fold more potency than ibrutinib in target organs, including PBMC and spleen.

Both in the REC-1 MCL and ABC subtype DLBCL (TMD-8) xenograft models, BGB-3111 induces dose-dependent anti-tumor effects and demonstrates superior efficacy in comparison with ibrutinib. Toxicity study in rats indicates that BGB-3111 is very well tolerated, and the MTD is not reached when it is dosed up to 250 mg/kg/day.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Cell-free assays
	濃度	0.3 nM
	反応時間
	実験の流れ
動物実験	動物モデル	NCG mice
	投薬量	2.5 mg/kg
	投与方法	i.v.

参考

http://www.bloodjournal.org/content/126/23/832?sso-checked=true
http://cancerres.aacrjournals.org/content/75/15_Supplement/2597
https://pubmed.ncbi.nlm.nih.gov/27590878/

https://pubmed.ncbi.nlm.nih.gov/31381333/

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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