2. PI3K/Akt/mTOR
  3. PI3K
  4. IHMT-PI3K-455

IHMT-PI3K-455 (Compound 15u) is a potent, selective, orally active PI3Kγ/δ dual inhibitor with IC50s of 7.1 nM and 0.57 nM for PI3Kγ and PI3Kδ, respectively. IHMT-PI3K-455 suppresses the AKT phosphorylation. IHMT-PI3K-455 inhibits tumor growth by recruiting and activating more CD8+ killing T cells.IHMT-PI3K-455 is used in cancer research.

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

IHMT-PI3K-455 Chemical Structure

IHMT-PI3K-455 Chemical Structure

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IHMT-PI3K-455 Related Antibodies

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Description

IHMT-PI3K-455 (Compound 15u) is a potent, selective, orally active PI3Kγ/δ dual inhibitor with IC50s of 7.1 nM and 0.57 nM for PI3Kγ and PI3Kδ, respectively. IHMT-PI3K-455 suppresses the AKT phosphorylation. IHMT-PI3K-455 inhibits tumor growth by recruiting and activating more CD8+ killing T cells.IHMT-PI3K-455 is used in cancer research[1].

IC50 & Target

PI3Kα

6.717 μM (IC50)

PI3Kβ

42.04 nM (IC50)

PI3Kγ

7.1 nM (IC50)

PI3Kδ

0.57 nM (IC50)

In Vitro

IHMT-PI3K-455 (1 μM, 2 h) suppresses the PI3Kγ/δ-mediated AKT phosphorylation in RAW264.7 cells and Raji cells[1].
IHMT-PI3K-455 (1 μM, 72 h) alters the macrophage polarization in M2 macrophages derived from THP-1 and BMDM cells[1].

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

IHMT-PI3K-455 Related Antibodies

Cell Differentiation Assay[1]

Cell Line: Macrophages
Concentration: 0.1, 1 μM
Incubation Time: 72 h
Result: Increased the proinflammatory M1 macrophage phenotype in a dose-dependent manner, with a concomitant dose-dependent decrease of the anti-inflammatory M2 macrophage phenotype.
Repolarized M2 phenotype toward M1 phenotype in THP-1 and BMDM macrophages.

Western Blot Analysis[1]

Cell Line: RAW264.7 cells; Raji cells
Concentration: 0, 0.01, 0.03, 0.1, 0.3, 1 μM
Incubation Time: 2 h
Result: Potently inhibited the PI3Kγ-mediated AKT473 phosphorylation in RAW264.7 cells (human C5a stimulation) with an IC50 value of 0.015 μM.
Potently inhibited the PI3Kδ-mediated AKT473 phosphorylation in Raji cells (anti-IgM stimulation) with an IC50 value of 0.010 μM.
In Vivo

IHMT-PI3K-455 (40 mg/kg for p.o; once daily for 30 days) inhibits the tumor growth in a MC38 tumor xenograft model[1].
IHMT-PI3K-455 (40 mg/kg for p.o; once daily for 30 days) inhibits tumor growth by recruiting and activating more CD8+ killing T cells[1].
Pharmacokinetic parameters of IHMT-PI3K-455 in Sprague-Dawley rats[1]

Dose (mg/kg) Administration route Cmax (ng/mL) Tmax (h) AUC0-∞ (h⋅ng/mL) T1/2 (h) CL (L/h/kg) Vz (L/kg) F (%)
1 i.v. 1233 0.03 477 1.59 2.12 4.80 –
10 p.o. 157 3.42 838 2.71 14.76 56.02 17.6

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

Animal Model: MC38 tumor model[1]
Dosage: 10 mg/kg, 40 mg/kg
Administration: Oral gavage (p.o.); Once daily for 30 days
Result: Significantly inhibited tumor size in a dose-dependent manner.
Increased tumor-infiltrating CD8+T cells.
Molecular Weight

517.49

Formula

C26H21F2N7O3
SMILES

COC1=C(OC)N=CC(C2=NC3=CC(NC4=CC=CC(CNC(C5=C(F)C=CC=C5F)=O)=N4)=NN3C=C2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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IHMT-PI3K-455 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IHMT-PI3K-455PI3KPhosphoinositide 3-kinaseCancerMC38 xenograft modelTHP-1BMDM macrophagesInhibitorinhibitorinhibit

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