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1305267-37-1

1305267-37-1 structure
1305267-37-1 structure
  • Name: MSC2360844
  • Chemical Name: MSC2360844
  • CAS Number: 1305267-37-1
  • Molecular Formula: C26H27FN4O5S
  • Molecular Weight: 526.58
  • Catalog: Signaling Pathways PI3K/Akt/mTOR PI3K
  • Create Date: 2020-04-13 21:47:04
  • Modify Date: 2024-09-18 11:00:17
  • MSC2360844 is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 shows highly selective against a panel of 278 additional kinases[1].

Name MSC2360844
Description MSC2360844 is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 shows highly selective against a panel of 278 additional kinases[1].
Related Catalog
Target

PI3Kδ:145 nM (IC50)

In Vitro MSC2360844 (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 inhibits B cell proliferation in a concentration-dependent manner with an IC50 of 48 nM. MSC2360844 blocks BCR- and TCR-mediated responses in lymphocytes and TLR-induced IFNα by pDC in human primary cells[1]. Cell Proliferation Assay[1] Cell Line: B cells Concentration: 0-10 μM Incubation Time: 1 hour Result: Inhibited B cell proliferation in a concentration-dependent manner with an IC50 of 48 nM.
In Vivo MSC2360844 (6.6-66 mg/kg; daily from week 2 to 10) ameliorates disease manifestations in a murine SLE model[1]. Animal Model: NZB/W F1 female mice[1] Dosage: 6.6, 22, or 66 mg/kg Administration: Oral; starting at week 2 post ADV-IFNα delivery, once daily at 10 weeks Result: Significantly reduced proteinuria incidence and severity in a dose-dependent manner.
References

[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.

Molecular Formula C26H27FN4O5S
Molecular Weight 526.58