BMS-986142
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $1750 | Check With Us |
| 500mg | $2350 | Check With Us |
| 1g | $3525 | Check With Us |
: Cat #: V4066 CAS #: 1643368-58-4 Purity ≥ 99%
Description: BMS-986142, a carbazole and tetrahydrocarbazole based compound, is a novel, potent and highly selective reversible Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 0.5 nM.
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| Molecular Weight (MW) | 572.61 |
|---|---|
| Molecular Formula | C32H30F2N4O4 |
| CAS No. | 1643368-58-4 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: ≥ 120 mg/mLr |
| Water: < 1mg/mLr | |
| Ethanol: N/A | |
| SMILES Code | O=C(C1=CC(F)=[C@]([C@]2=CC=CC(N3C(N(C)C4=C(C=CC=C4F)C3=O)=O)=C2C)C5=C1NC6=C5CC[C@H](C(C)(O)C)C6)N |
| Synonyms | BMS-986142; BMS 986142; BMS986142 |
| Protocol | In Vitro | BMS-986142 potently inhibits human recombinant BTK with an IC50 of 0.5 nM in enzymatic assays. Against a panel of 384 kinases, BMS-986142 is highly selective, with only five other kinases (Tec, ITK, BLK, Txk, BMX) inhibited with <100-fold selectivity for BTK. Four of these kinases are Tec family kinases, of which BTK is a member, and only Tec (IC50=10 nM) is inhibited with <30-fold selectivity compared with BTK. BMS-986142 does not inhibit CD40L-induced expression of CD86 or CD69 on peripheral blood B cells (IC50>10,000 nM for both). When Ramos B cells are treated with anti-IgM to activate BCR, BMS-986142 inhibits BTK-dependent calcium flux with an IC50 of 9 nM. |
|---|---|---|
| In Vivo | BMS-986142 at 4, 10, and 30 mg/kg results in dose-dependent reductions of 26%, 43%, and 79% in clinically evident disease, respectively, at the end of the study. Interestingly, 4 mg/kg BMS-986142 provides an additive benefit in clinical scores (54% inhibition) when co-administered with MTX versus 19% inhibition with MTX alone. Co-administration of BMS-986142 at 4 mg/kg with MTX result in a 53% reduction in inflammation and bone resorption compared with 24% and 10%, respectively, with either drug alone. Furthermore, serum anti-collagen II IgG titers are significantly inhibited with 10 and 30 mg/kg BMS-986142. BMS-986142 also produces dose-dependent reductions in clinical scores when administration is delayed until the collagen booster on day 21. BMS-986142 doses of 2, 4, and 25 mg/kg in this therapeutic dosing regimen result in clinical score reductions of 17%, 37%, and 67%, respectively, at the end of the study. |
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 | 1.7464 mL | 8.7319 mL | 17.4639 mL | 34.9278 mL |
| 5mM | 0.3493 mL | 1.7464 mL | 3.4928 mL | 6.9856 mL |
| 10mM | 0.1746 mL | 0.8732 mL | 1.7464 mL | 3.4928 mL |
| 20mM | 0.0873 mL | 0.4366 mL | 0.8732 mL | 1.7464 mL |
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