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[CAS NO. 1510829-06-7] Vecabrutinib
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-109078 |
| Brand: | MCE |
| CAS: | 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 |
2 Publications Citing Use of MCE
Summary
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
DMSO : 125 mg/mL ( 235.88 mM ; Need ultrasonic)
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 |
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1.
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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.
-
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
References
- [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] 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
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