1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. Zanubrutinib

Zanubrutinib (Synonyms: BGB-3111)

製品番号: HY-101474A 純度: 98.33% ee.: 98.54%
取扱説明書

Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor.

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Zanubrutinib 構造式

Zanubrutinib 構造式

CAS 番号 : 1691249-45-2

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 187 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 180 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 320 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 720 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1300 在庫あり
Estimated Time of Arrival: December 31
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

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製品説明

Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor[1].

IC50 & Target

BTK[1]

体外実験

Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (BTK) inhibitor. In both biochemical and cellular assays, Zanubrutinib demonstrates nanomolar BTK inhibition activity. In several MCL and DLBCL cell lines, Zanubrutinib inhibits BCR aggregation-triggered BTK autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation. In comparison with PCI-32765, Zanubrutinib shows much more restricted off-target activities against a panel of kinases, including ITK[1].

体内実験

Zanubrutinib (BGB-3111) induces dose-dependent anti-tumor effects against REC-1 MCL xenografts engrafted either subcutaneously or systemically via tail vein injection in mice. In the subcutaneous xenografts, Zanubrutinib at 2.5 mg/kg BID shows similar activity as PCI-32765 at 50 mg/kg QD. In the systemic model, the median survival of Zanubrutinib 25 mg/kg BID group is significantly longer than those of both PCI-32765 50 mg/kg QD and BID groups. In an ABC-subtype DLBCL (TMD-8) subcutaneous xenograft model, Zanubrutinib also demonstrates better anti-tumor activity than PCI-32765. Preliminary 14-day toxicity study in rats shows that Zanubrutinib is very well tolerated and maximal tolerate dose (MTD) is not reached when it is dosed up to 250 mg/kg/day[1].

臨床実験
分子量

471.55

分子式

C₂₇H₂₉N₅O₃

CAS 番号

1691249-45-2

SMILES

NC(C1=C2N(N=C1C3=CC=C(OC4=CC=CC=C4)C=C3)[[email protected]](C5CCN(C(C=C)=O)CC5)CCN2)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 56.75 mg/mL (120.35 mM)

Ethanol : < 1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1207 mL 10.6033 mL 21.2067 mL
5 mM 0.4241 mL 2.1207 mL 4.2413 mL
10 mM 0.2121 mL 1.0603 mL 2.1207 mL
*Please refer to the solubility information to select the appropriate solvent.
参考文献
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Keywords:

ZanubrutinibBGB-3111BGB3111BGB 3111BtkBruton tyrosine kinaseInhibitorinhibitorinhibit

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製品名:
Zanubrutinib
製品番号:
HY-101474A
数量:
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