Description
BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC50 of 1 nM and a Kd of 0.3 nM. BIIB068 shows more >400-fold selective for BTK than other kinases. BIIB068 has the potential for autoimmune diseases research.
Product information
CAS Number: 1798787-27-5
Molecular Weight: 435.52
Formula: C23H29N7O2
Chemical Name: N-[(2-methyl-4-{2-[(1-methyl-1H-pyrazol-4-yl)amino]pyrimidin-4-yl}phenyl)methyl]-3-(propan-2-yloxy)azetidine-1-carboxamide
Smiles: CN1C=C(C=N1)NC1=NC(=CC=N1)C1=CC=C(CNC(=O)N2CC(C2)OC(C)C)C(C)=C1
InChiKey: BMWMKGNVAMXXCH-UHFFFAOYSA-N
InChi: InChI=1S/C23H29N7O2/c1-15(2)32-20-13-30(14-20)23(31)25-10-18-6-5-17(9-16(18)3)21-7-8-24-22(28-21)27-19-11-26-29(4)12-19/h5-9,11-12,15,20H,10,13-14H2,1-4H3,(H,25,31)(H,24,27,28)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 31.25 mg/mL (71.75 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
BIIB068 (compound 1) improves the whole blood cell potency (human whole blood BTK phosphorylation (IC50 = 0.12 µM). BIIB068 (compound 1; 30 µM,10 µM, 3.3 µM, and 1.1 µM) inhibits BCR mediated PLCγ2 phosphorylation in Ramos B cells (IC50= 0.4 µM), anti-IgD induced and anti-IgM BCR-induced B cell activation in human PBMCs (IC50 = 0.11 µM and 0.21 µM, respectively). BIIB068 (compound 1) inhibits FcγR-mediated ROS production in neutrophils with an IC50 of 54 nM.
In Vivo:
BIIB068 (compound 1) is stable in the plasma of mouse, rat, beagle dog, and cynomolgus monkey (>95% parent compound remaining after 6 hours of incubation). BIIB068 (compound 1) exhibits good drug-like properties (LLE = 5) which results in low in vivo clearance (CL %Qh = 6) and moderate oral bioavailability (%F = 48) when dosed in rats. BIIB068 (5 mg/kg; po) treatment shows the T1/2 of 1.2 hours, 2.1 hours and 0.9 hour for rats, dog and cynomolgus monkey, respectively. BIIB068 shows acceptable ADME (absorption, distribution, metabolism, and excretion) properties.
Products are for research use only. Not for human use.
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