1. PI3K/Akt/mTOR
  2. PI3K
  3. PI3Kδ-IN-8

PI3Kδ-IN-8 

Cat. No.: HY-134472
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PI3Kδ-IN-8 is a potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 3.3 nM. PI3Kδ-IN-8 shows selectivity for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50=377.2, 241.6, 17.9 nM, respectively). PI3Kδ-IN-8 has anti-tumor activity.

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

PI3Kδ-IN-8 Chemical Structure

PI3Kδ-IN-8 Chemical Structure

CAS No. : 2101518-75-4

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Description

PI3Kδ-IN-8 is a potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 3.3 nM. PI3Kδ-IN-8 shows selectivity for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50=377.2, 241.6, 17.9 nM, respectively). PI3Kδ-IN-8 has anti-tumor activity[1].

IC50 & Target[1]

PI3Kδ

3.3 nM (IC50)

PI3Kγ

17.9 nM (IC50)

PI3Kβ

241.6 nM (IC50)

PI3Kα

377.2 nM (IC50)

In Vitro

PI3Kδ-IN-8 (compound 34) (0.1 nM-10 μM; 96 h) shows excellent potency against representative DLBCL cell lines, of either GCB (SUDHL-6), or ABC subtype (OCI-Ly10 and TMD-8)[1].
PI3Kδ-IN-8 (1 h) inhibits the PI3K-induced AKT phosphorylation in anti-IgM stimulated Raji cells, with an IC50 of 9.5 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: SUDHL-6, OCI-Ly10, and TMD-8 cell lines
Concentration: 0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time: 96 hours
Result: Inhibited the viability of SUDHL-6, OCI-Ly10, and TMD-8 cells, with IC50s of <0.1 nM, <1 nM, and <0.1 nM, respectively.
In Vivo

PI3Kδ-IN-8 (1-30 mg/kg; p.o. once daily for 24 d) significantly reduces the tumor volume and tumor weight in a dose-dependent manner in mice[1].
PI3Kδ-IN-8 (1 mg/kg; i.v.) displays a suitable half-life (1 h), Cmax (2.3 μM) and low clearance (5.6 mL/min/kg) in mice[1].
PI3Kδ-IN-8 (10 mg/kg; p.o.) displays moderate oral bioavailability (39%), Cmax (7.5 μM), and AUClast(22 μM•h) in mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NOD scid mice were injected OCI-Ly10 cells[1]
Dosage: 1, 3, 10, 30 mg/kg
Administration: P.o. once daily for 24 days
Result: Reduced the tumor volume, with an ED50 of 6.47 mg/kg.
Tumor growth inhibition of 81.95% was seen with a highly significant reduction in both tumor volume and tumor weight.
Animal Model: Male BALB/c mice[1]
Dosage: 1 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: I.v.: t1/2=1 h, Cmax=2.3 μM, CL=5.6 mL/min/kg.
P.o.: F=39%, Cmax=7.5 μM, AUClast=22μM•h.
Molecular Weight

509.51

Formula

C₂₈H₂₁F₂N₇O

CAS No.
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PI3Kδ-IN-8
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