(±)-Zanubrutinib (Synonyms: (±)-BGB-3111)

Cat. No.: HY-101474 Purity: 99.70%: Data Sheet SDS Handling Instructions

(±)-Zanubrutinib is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.

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

(±)-Zanubrutinib Chemical Structure

CAS No. : 1633350-06-7

Size	Price	Stock
10 mM * 1 mL in DMSO	USD 145	In-stock
1 mg	USD 90	In-stock
5 mg	USD 140	In-stock
10 mg	USD 220	In-stock
50 mg	USD 880	In-stock
100 mg	USD 1400	In-stock
200 mg		Get quote
500 mg		Get quote

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Customer Review

Other Forms of (±)-Zanubrutinib:

Zanubrutinib In-stock
(R)-Zanubrutinib In-stock

Customer Validation

•Dr. Wang from Chinese Academy of Sciences.

: (±)-Zanubrutinib purchased from MCE. Usage Cited in: Dr. Wang from Chinese Academy of Sciences.; Determining IC₅₀ for Zanubrutinib. IC₅₀ values for Zanubrutinib are determined using the ADP-Glo^™ Kinase Assay. Curve fitting is performed using GraphPad Prism sigmoidal dose-response (variable slope) software.

: (±)-Zanubrutinib purchased from MCE. Usage Cited in: Dr. Wang from Chinese Academy of Sciences.; Determining IC₅₀ for Zanubrutinib. IC₅₀ values for Zanubrutinib are determined using the ADP-Glo^™ Kinase Assay. Curve fitting is performed using GraphPad Prism sigmoidal dose-response (variable slope) software.

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Description	(±)-Zanubrutinib is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
In Vitro	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. (±)-Zanubrutinib is at least 10-fold weaker than ibrutinib in inhibiting rituximab induced ADCC, consistent with its weak ITK inhibition activity^[1].
In Vivo	(±)-Zanubrutinib 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. 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 250mg/kg/day^[1].
References	[1]. Na L, et al. BGB-3111 is a novel and highly selective Bruton's tyrosine kinase (BTK) inhibitor. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2597. doi:10.1158/1538-7445.AM2015-2597

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

[1]. Na L, et al. BGB-3111 is a novel and highly selective Bruton's tyrosine kinase (BTK) inhibitor. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2597. doi:10.1158/1538-7445.AM2015-2597

Molecular Weight

471.55

Formula

C₂₇H₂₉N₅O₃

CAS No.

1633350-06-7

SMILES

NC(C1=C2N(N=C1C3=CC=C(OC4=CC=CC=C4)C=C3)C(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

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

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(±)-Zanubrutinib (Synonyms: (±)-BGB-3111)

Customer Review

Other Forms of (±)-Zanubrutinib:

Customer Validation

Featured Recommendations

•Related Small Molecules:

Biological Activity

Protocol

Technical Information

Purity & Documentation

References