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BMS-935177 BTK inhibitor

Name: BMS-935177
Brand: Selleck Chemicals
SKU: S8348
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S8348

BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which this compound is between 5- and 67-fold selective.

Chemical Structure

Molecular Weight: 502.56

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	EGFR VEGFR JAK PDGFR FGFR Src FLT3 HER2 Bcr-Abl HIF ALK Syk FAK VDA
Related Products	Spebrutinib (AVL-292) tirabrutinib(ONO-4059) hydrochloride CGI1746 LFM-A13 CNX-774 Fenebrutinib (GDC-0853) Branebrutinib (BMS-986195) Evobrutinib BMS-986142 Nemtabrutinib (ARQ 531) Pirtobrutinib (LOXO-305)

Chemical Information, Storage & Stability

Molecular Weight	502.56	Formula	C₃₁H₂₆N₄O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1231889-53-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(C=CC=C1N2C=NC3=CC=CC=C3C2=O)C4=C5C6=C(C=C(C=C6)C(C)(C)O)NC5=C(C=C4)C(=O)N

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (198.98 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	BTK ^[1] (Cell-free assay) 2.8 nM TEC ^[1] (Cell-free assay) 13 nM BLK ^[1] (Cell-free assay) 20 nM BMX ^[1] (Cell-free assay) 24 nM TrkA ^[1] (Cell-free assay) 30 nM HER4 ^[1] (Cell-free assay) 50 nM ITK ^[1] (Cell-free assay) 96 nM TrkB ^[1] (Cell-free assay) 100 nM RET ^[1] (Cell-free assay) 110 nM LCK ^[1] (Cell-free assay) 150 nM Lyn ^[1] (Cell-free assay) 160 nM TXK ^[1] (Cell-free assay) 180 nM
In vitro	BMS-935177 shows greater than 50-fold selectivity over the SRC family of kinases, including 1100-fold selectivity over SRC itself. Other kinases inhibited with a potency less than 150 nM (50-fold selectivity) included TRKA, HER4, TRKB, and RET. It inhibits calcium flux in human Ramos B cells (IC50 = 27 nM) and inhibits CD69 surface expression in peripheral B cells stimulated with anti-IgM and anti-IgG. However, this compound has no effect on CD69 surface expression in B cells stimulated through the CD40 receptor with CD40 ligand. Against IgG-containing immune complex-driven low affinity activating Fcγ receptor (FcγRIIa and FcγRIII) end points in peripheral blood mononuclear cells (PBMCs), this chemical effectively inhibited TNFα production with an IC50 value of 14 nM^[1].
In vivo	Plasma protein binding for BMS-935177 is high for all species, with less than 1% free for human. It has excellent oral bioavailability in all preclinical species, from both suspension and solution dosing, despite its low aqueous solubility. The oral bioavailability for this compound with solution dosing ranges from 84% to 100% in rat, mouse, dog, and cynomolgus monkey, with low clearance in single intravenous (iv) infusion studies. When dosed at 2 mg/kg i.v. in mouse and rat, the T_1/2 of this chemical is 4 h and 5.1 h respectively^[1].
References	https://pubmed.ncbi.nlm.nih.gov/27531604/

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