Product Name :
BIIB068
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.
CAS:
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)
Purity:
≥98% (or refer to the Certificate of Analysis)
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.
Additional information:
BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC50 of 1 nM and a Kd of 0.{{Pritelivir} site|{Pritelivir} Anti-infection|{Pritelivir} Biological Activity|{Pritelivir} Data Sheet|{Pritelivir} manufacturer|{Pritelivir} Epigenetic Reader Domain} 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.{{Fmoc-Arg(Pbf)-OH} medchemexpress|{Fmoc-Arg(Pbf)-OH} {Amino Acid Derivatives}|{Fmoc-Arg(Pbf)-OH} Protocol|{Fmoc-Arg(Pbf)-OH} In Vitro|{Fmoc-Arg(Pbf)-OH} custom synthesis|{Fmoc-Arg(Pbf)-OH} Autophagy} 3 µM, and 1.PMID:23522542 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.|