1. Protein Tyrosine Kinase/RTK
  2. Btk

Zanubrutinib (Synonyms: BGB-3111)

Cat. No.: HY-101474A Purity: 99.45%
Handling Instructions

Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.

For research use only. We do not sell to patients.

Zanubrutinib Chemical Structure

Zanubrutinib Chemical Structure

CAS No. : 1691249-45-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 508 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
1 mg USD 190 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 490 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 790 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 1900 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Other Forms of Zanubrutinib:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.

IC50 & Target

BTK[1]

In Vitro

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 ibrutinib, Zanubrutinib shows much more restricted off-target activities against a panel of kinases, including ITK[1].

In Vivo

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 ibrutinib 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 ibrutinib 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 ibrutinib. 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].

References
Preparing Stock Solutions
Concentration Volume 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.
References
Molecular Weight

471.55

Formula

C₂₇H₂₉N₅O₃

CAS No.

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 56.75 mg/mL; Methanol: < 1 mg/mL; Ethanol: < 1 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Zanubrutinib
Cat. No.:
HY-101474A
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