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BMS-935177

Catalog No. T14681 CAS 1231889-53-4

BMS-935177 is a reversible BTK inhibitor with IC50 value of 3 nM.

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BMS-935177, CAS 1231889-53-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 61.00
2 mg	In stock	$ 89.00
5 mg	In stock	$ 178.00
10 mg	In stock	Inquiry
50 mg	In stock	Inquiry
1 mL * 10 mM (in DMSO)	In stock	$ 206.00

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Purity: 99.89%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BMS-935177 is a reversible BTK inhibitor with IC50 value of 3 nM.
Targets&IC50	BTK:3 nM
In vitro	In human Ramos B cells, BMS-935177 inhibits calcium flux with an IC50 of 27 nM. BMS-935177 inhibits CD69 surface expression in peripheral B cells stimulated with antiIgM and anti-IgG. Against IgG-containing immune complexdriven low affinity activating FcγRIIa and FcγRIII end points in peripheral blood mononuclear cells, BMS-935177 effectively inhibits TNFα production (IC50 = 14 nM). BMS-935177 shows mean IC50 values of 550 and 2060 nM in human and mouse whole blood, respectively[1].
In vivo	BMS-935177(5, 20, and 45 mg/kg) inhibits anti-KLH antibodies of the IgG isotype at day 14, with statistically significant reductions at all doses. In satellite mice, BMS-935177 (5 mg/kg) maintains the plasma concentration above the mouse whole blood BCR-stimulated CD69 IC50 value of 2 μM for only 5 h. BMS-935177(10, 20, and 30 mg/kg) provides dose-dependently reduces both the severity and incidence of clinically evident disease in this rodent model of RA. BMS-935177(10 mg/kg) reduces the disease severity about 40%, and the percentage of animals showing any signs of disease is reduced by a third[1].

Molecular Weight	502.56
Formula	C31H26N4O3
CAS No.	1231889-53-4

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 117mg/mL (232.8mM)

References and Literature

1. De Lucca GV, et al. Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177). J Med Chem. 2016 Sep 8;59(17):7915-35.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BMS-935177 1231889-53-4 Angiogenesis Tyrosine Kinase/Adaptors BTK BMS935177 BMS 935177 inhibitor inhibit

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