| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C26H21F2N7O3 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
IHMT-PI3K-455 is a potent, selective, orally active dual inhibitor of PI3Kγ and PI3Kδ, with IC50 values of 7.1 nM and 0.57 nM, respectively. It suppresses AKT phosphorylation and inhibits tumor growth by recruiting and activating more CD8+ killer T cells, and it is used in cancer research[1]. It has the molecular formula C26H21F2N7O3 and a molecular weight of 517.49 g/mol.
Physical & Chemical Properties
| CAS Number | 3047746-40-4 |
|---|---|
| Molecular Formula | C26H21F2N7O3 |
| Molecular Weight | 517.49 g/mol |
| SMILES | COC1=C(OC)N=CC(C2=NC3=CC(NC4=CC=CC(CNC(C5=C(F)C=CC=C5F)=O)=N4)=NN3C=C2)=C1 |
| Target | PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ |
| Signaling Pathway | PI3K/Akt/mTOR |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
|
PI3Kα 6.717 μM (IC50) |
PI3Kβ 42.04 nM (IC50) |
PI3Kγ 7.1 nM (IC50) |
PI3Kδ 0.57 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
In RAW264.7 and Raji cells, IHMT-PI3K-455 (1 μM, 2 h) suppresses PI3Kγ/δ-mediated AKT phosphorylation[1]. IHMT-PI3K-455 (1 μM, 72 h) changes macrophage polarization in M2 macrophages derived from THP-1 and BMDM cells[1].
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 dosed at 40 mg/kg p.o. once daily for 30 days inhibits tumor growth in a MC38 tumor xenograft model[1]. At 40 mg/kg p.o. once daily for 30 days, IHMT-PI3K-455 acts through recruitment and activation of more CD8+ killing T cells, inhibiting tumor growth[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 |
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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