[CAS NO. 1510829-06-7] Vecabrutinib

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PRODUCTS SPECIFICATIONS [1510829-06-7]

Catalog

HY-109078

Brand

MCE

CAS

1510829-06-7

DESCRIPTION [1510829-06-7]

Overview

MDL	-
Molecular Weight	529.92
Molecular Formula	C22H24ClF4N7O2
SMILES	NC([C@@H]1[C@@H](N(CCC[C@H]2NC3=CC(C(F)(F)F)=CC(Cl)=C3)C2=O)CN(C4=NC=NC(N)=C4F)CC1)=O

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

2 Publications Citing Use of MCE

Summary

Vecabrutinib (SNS-062) is a potent, noncovalent BTK and ITK inhibitor, with K _d values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib shows an IC ₅₀ of 24 nM for ITK ^[1] ^[2] .

IC50 & Target

IC50: 24 nM (ITK) ^[2]
Kd: 0.3 nM (BTK), 2.2 nM (ITK) ^[1]

In Vitro

Vecabrutinib inhibits pBTK in human whole blood with an average IC ₅₀ of 50 nM. Vecabrutinib inhibits WT and C481S BTK with similar IC ₅₀ s (pBTK IC ₅₀ s: WT BTK 2.9 nM, C481S BTK 4.4 nM) ^[1] . In a recombinant kinase assay, IC ₅₀ s 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 is six times more potent than PCI-32765 and greater than 640 times more potent than acalabrutinib against C481S BTK. Vecabrutinib demonstrates dose-dependent inhibition of BTK in primary patient CLL cells comparable to PCI-32765 via immunoblot for BTK phosphorylation. Vecabrutinib decreases viability of primary CLL cells in the presence of HS5 stromal protection by 5.5% ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Vecabrutinib has good oral bioavailability in rat and dog (%F ≥ 40%) and a terminal half-life of 5 to 6 hours. Vecabrutinib is well tolerated with continuous drug levels and at exposures much greater than those achieved for PCI-32765 ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03037645	Sunesis Pharmaceuticals	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma\|Lymphoplasmacytoid Lymphoma\|Mantle-Cell Lymphoma\|Waldenstrom Macroglobulinemia\|Diffuse Large B Cell Lymphoma\|Follicular Lymphoma\|Marginal Zone Lymphoma	April 28, 2017	Phase 1\|Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 235.88 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8871 mL	9.4354 mL	18.8708 mL
5 mM	0.3774 mL	1.8871 mL	3.7742 mL
10 mM	0.1887 mL	0.9435 mL	1.8871 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 2.5 mg/mL (4.72 mM); Clear solution
2.

Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.72 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (3.93 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (3.93 mM); Clear solution
5.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.93 mM); Clear solution

* All of the co-solvents are available by MCE.