1. PI3K/Akt/mTOR
  2. PI3K
  3. MSC2360844

MSC2360844 

Cat. No.: HY-135827
Handling Instructions

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.

For research use only. We do not sell to patients.

MSC2360844 Chemical Structure

MSC2360844 Chemical Structure

CAS No. : 1305267-37-1

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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].

IC50 & 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.
Molecular Weight

526.58

Formula

C₂₆H₂₇FN₄O₅S

CAS No.

1305267-37-1

SMILES

O=C(C1=NN(C2=CC=C(CN3CCOCC3)C=C2)C(C4=CC=CC(F)=C45)=C1CS5(=O)=O)N6CCOCC6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

MSC2360844MSC 2360844MSC-2360844PI3KPhosphoinositide 3-kinaseBcellsSLE-pronefunctionsproliferationprimaryInhibitorinhibitorinhibit

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MSC2360844
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