BMS-935177
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
100mg | $1550 | To Be Confirmed |
250mg | $2350 | To Be Confirmed |
500mg | $3965 | To Be Confirmed |
Cat #: V3184 CAS #: 1231889-53-4 Purity ≥ 98%
Description: BMS-935177 is a potent, selective, reversible, and 2nd generation inhibitor of Bruton’s Tyrosine Kinase (BTK) with an IC50 of 3 nM.
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Molecular Weight (MW) | 502.56 |
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Molecular Formula | C31H26N4O3 |
CAS No. | 1231889-53-4 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: >100 mg/mLr |
Water: < 1 mg/mLr | |
Ethanol: >100 mg/mL | |
SMILES Code | O=C(C1=CC=C(C2=CC=CC(N3C(C4=C(C=CC=C4)N=C3)=O)=C2C)C5=C1NC6=C5C=CC(C(C)(O)C)=C6)N |
Synonyms | BMS-935177; BMS935177; BMS 935177 |
Protocol | In Vitro | In B cells stimulated through the BCR, BMS-935177 selectively inhibits several different readouts. BMS-935177 inhibits calcium flux in human Ramos B cells (IC50=27 nM) and inhibits CD69 surface expression in peripheral B cells stimulated with antiIgM and anti-IgG. However, BMS-935177 has no effect on CD69 surface expression in B cells stimulated through the CD40 receptor with CD40 ligand. Against IgG-containing immune complexdriven low affinity activating Fcγ receptor (FcγRIIa and FcγRIII) end points in peripheral blood mononuclear cells (PBMCs), BMS-935177 effectively inhibits TNFα production with an IC50 value of 14 nM. BMS-935177 shows mean IC50 values of 550±100 (n=11) and 2060±240 nM (n=3) in human and mouse whole blood, respectively. |
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In Vivo | When dosed orally once daily at 5, 20, and 45 mg/kg to mice, BMS-935177 inhibits anti-KLH antibodies of the IgG isotype at day 14, with statistically significant reductions at all doses. In satellite mice from this study dosed with 6 at 5 mg/kg, the plasma concentration is maintained above the mouse whole blood BCR-stimulated CD69 IC50 value of 2 μM for only approximately 5 h. At once daily oral doses of 10, 20, and 30 mg/kg beginning on the day of primary immunization, BMS-935177 provides a clear dose-dependent reduction in both the severity and incidence of clinically evident disease in this rodent model of RA. At 10 mg/kg of BMS-935177, disease severity is reduced about 40% compared to vehicle treatment, and the percentage of animals showing any signs of disease is reduced by a third. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.9898 mL | 9.9491 mL | 19.8981 mL | 39.7962 mL |
5mM | 0.3980 mL | 1.9898 mL | 3.9796 mL | 7.9592 mL |
10mM | 0.1990 mL | 0.9949 mL | 1.9898 mL | 3.9796 mL |
20mM | 0.0995 mL | 0.4975 mL | 0.9949 mL | 1.9898 mL |
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Method for preparing in vivo formulation:
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Tween 80,mix and clarify, next add
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