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Vecabrutinib

Catalog No. T17220 CAS 1510829-06-7

Synonyms: SNS-062

Vecabrutinib (SNS-062) is a potent and noncovalent BTK and ITK inhibitor (Kd: 0.3 nM and 2.2 nM, respectively). Vecabrutinib displays an IC50 of 24 nM for ITK.

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Vecabrutinib, CAS 1510829-06-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 132.00
5 mg	In stock	$ 328.00
10 mg	In stock	$ 538.00
25 mg	In stock	$ 873.00
50 mg	In stock	$ 1,180.00
100 mg	In stock	$ 1,620.00
1 mL * 10 mM (in DMSO)	In stock	$ 385.00

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Purity: 100%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Vecabrutinib (SNS-062) is a potent and noncovalent BTK and ITK inhibitor (Kd: 0.3 nM and 2.2 nM, respectively). Vecabrutinib displays an IC50 of 24 nM for ITK.
Targets&IC50	BTK:（kd）0.3 nM, ITK:2.2 nM（kd）, ITK:24 nM
In vitro	Vecabrutinib is six times more potent than PCI-32765 and greater than 640 times more potent than acalabrutinib against C481S BTK. Vecabrutinib inhibits pBTK in human whole blood (average IC50: 50 nM). Vecabrutinib inhibits WT and C481S BTK with similar IC50s (pBTK IC50s: 2.9 nM and 4.4 nM for WT BTK and C481S BTK). In a recombinant kinase assay, IC50s of Vecabrutinib against WT BTK and C481S BTK are 4.6 nM and 1.1 nM. Vecabrutinib retains activity against the mutated BTK variant. Vecabrutinib demonstrates dose-dependent inhibition of BTK in primary patient CLL cells comparable to PCI-32765 via immunoblot for BTK phosphorylation. Vecabrutinib decreases the viability of primary CLL cells in the presence of HS5 stromal protection by 5.5% [1][2].
In vivo	Vecabrutinib is well tolerated with continuous drug levels. Vecabrutinib has good oral bioavailability in rat and dog (%F ≥ 40%) and a terminal half-life of 5 to 6 hours [1].

Synonyms	SNS-062
Molecular Weight	529.92
Formula	C22H24ClF4N7O2
CAS No.	1510829-06-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 112.5 mg/mL (212.3 mM), Sonication is recommended.

References and Literature

1. Minke E. Binnerts, et al. Abstract C186: SNS-062 is a potent noncovalent BTK inhibitor with comparable activity against wild type BTK and BTK with an acquired resistance mutation. Molecular Cancer Therapeutics. December 2015 Volume 14, Issue 12 Supplement 2 2. Catherine A. Fabian, et al. Abstract 1207: SNS-062 demonstrates efficacy in chronic lymphocytic leukemia in vitro and inhibits C481S mutated Bruton tyrosine kinase. Cancer Research July 2017 Volume 77, Issue 13 Supplement

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Covalent Inhibitor Library Anti-Cancer Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

Vecabrutinib 1510829-06-7 Angiogenesis Tyrosine Kinase/Adaptors BTK Tyrosine Kinases SNS 062 SNS-062 SNS062 inhibitor inhibit

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