Vecabrutinib

SKU: orb1706486

Description

Vecabrutinib (SNS-062) is a potent, noncovalent dual inhibitor of BTK and ITK with respective Kd values of 0.3 nM and 2.2 nM, and an IC50 of 24 nM against ITK. This investigational compound is utilized in preclinical research for studying B-cell and T-cell signaling pathways in both in vitro and in vivo models of autoimmune and hematological disorders.

Research Area

Cardiovascular Research, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	1510829-06-7
MW	529.92
Purity	>99.99% (May vary between batches)
Formula	C₂₂H₂₄ClF₄N₇O₂
SMILES	NC(=O)[C@H]1CCN(C[C@@H]1N1CCC[C@@H](Nc2cc(Cl)cc(c2)C(F)(F)F)C1=O)c1ncnc(N)c1F
Target	BTK,Tyrosine Kinases
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.55 mM);DMSO:112.5 mg/mL (212.3 mM)

Bioactivity

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Target IC50	BTK:（kd）0.3 nM\|ITK:2.2 nM（kd）\|ITK:24 nM
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 . Read more...
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% . Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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BTK, ITK, TyrosineKinases, Tyrosine Kinases, Vecabrutinib, SNS 062, SNS062, SNS-062

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Compound Identifiers

PubChem CID

72547837 ↗

Key Properties

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No computed properties available.

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Vecabrutinib (orb1706486)

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Vecabrutinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

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Protocol Information

Vecabrutinib (orb1706486)

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