| Bioactivity | MSC2360844 hemifumarate is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 hemifumarate shows highly selective against a panel of 278 additional kinases[1]. |
| Invitro | MSC2360844 hemifumarate (0-10 μM; 1 hours) completely abolished BCR-induced pAkt in Ramos B cells in a concentration-dependent manner with IC50 values of 280 nM[1]. MSC2360844 hemifumarate inhibits B cell proliferation in a concentration-dependent manner with an IC50 of 48 nM. MSC2360844 hemifumarate blocks BCR- and TCR-mediated responses in lymphocytes and TLR-induced IFNα by pDC in human primary cells[1]. Cell Viability Assay[1] Cell Line: |
| In Vivo | MSC2360844 hemifumarate (6.6-66 mg/kg; daily from week 2 to 10) ameliorates disease manifestations in a murine SLE model[1]. Animal Model: |
| Name | MSC2360844 hemifumarate |
| CAS | 1621688-31-0 |
| Formula | C26H27FN4O5S.1/2C4H4O4 |
| Molar Mass | 584.62 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Haselmayer P, et al. Characterization of Novel PI3Kδ Inhibitors as Potential Therapeutics for SLE and Lupus Nephritis in Pre-Clinical Studies. Front Immunol. 2014 May 22;5:233. |
MSC2360844 hemifumarate
CAS: 1621688-31-0 F: C26H27FN4O5S.1/2C4H4O4 W: 584.62
MSC2360844 hemifumarate is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 he
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