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Chemical Structure : BIIB091
CAS No.: 2247614-80-6
Catalog No.: PC-72229Not For Human Use, Lab Use Only.
BIIB091 (BIIB 091) is a novel potent, selective, reversible BTK inhibitor with IC50 of 0.45 nM in enzymatic assays.
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|---|---|---|---|
| 2 mg | $398 | In stock | |
| 5 mg | $598 | In stock | |
| 10 mg | $958 | In stock | |
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| 100 mg | Get quote |
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BIIB091 (BIIB 091) is a novel potent, selective, reversible BTK inhibitor with IC50 of 0.45 nM in enzymatic assays.
BIIB091 demonstrated > 500-fold selectivity for BTK relative to all other kinases from a panel of >400 individual kinases evaluated in the DiscoverX KINOMEscan.
BIIB091 inhibited CD69 induction in anti-BCR-stimulated B cells in a dose‐dependent manner in PBMCs (IC50=5.4 nM) and in mouse splenocytes (IC50=16 nM).
BIIB091 blocks B‐cell proliferation and antigen-presenting functions in vitro and the associated B‐cell activation transcriptional programme, effectively blocks BCR-mediated antigen presentation to T cells and blocks myeloid cell functions in vitro.
BIIB091 blocks B-cell activation and differentiation into antibody-secreting and germinal center B cells in vivo, also demonstrates complete inhibition of B-cell activation over the dosing interval in a human phase 1 trial.
| M.Wt | 541.66 | |
| Formula | C29H35N9O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO (5.4 mg/mL) |
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| Chemical Name/SMILES |
1H-1,2,3-Triazole-4-carboxamide, 1-(1,1-dimethylethyl)-N-[(5R)-2,3,4,5-tetrahydro-8-[2-[(1-methyl-1H-pyrazol-4-yl)amino]-4-pyrimidinyl]-2-(3-oxetanyl)-1H-2-benzazepin-5-yl] |
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1. Hopkins BT, et al. J Med Chem. 2022 Jan 27;65(2):1206-1224.
2. Bame E, et al. Clin Transl Immunology. 2021 Jun 14;10(6):e1295.
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