AM-8508

Cat. No.: HY-120116: Data Sheet Handling Instructions
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AM-8508 is an orally bioactive PI3Kδ inhibitor with an IC₅₀ of 0.016 μM. AM-8508 selectively inhibits PI3Kδ, thereby blocking AKT phosphorylation mediated by the B cell receptor. AM-8508 suppresses the formation of antigen-specific IgG and IgM in rats immunized with keyhole limpet hemocyanin. AM-8508 can be used for the research of inflammatory diseases.

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

AM-8508 Chemical Structure

CAS No. : 1338483-67-2

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

PI3Kδ

0.016 μM (IC₅₀)

PI3Kα

58.2 μM (IC₅₀)

PI3Kβ

1.78 μM (IC₅₀)

PI3Kγ

5.8 μM (IC₅₀)

In Vitro

AM-8508 (Compound 1) potently and selectively inhibits the PI3Kδ subtype with an IC₅₀ of 0.016 μM, exhibiting 3638-fold, 111-fold and 363-fold selectivity over PI3Kα (IC₅₀ = 58.2 μM), PI3Kβ (IC₅₀ = 1.78 μM) and PI3Kγ (IC₅₀ = 5.8 μM), respectively^[1].
AM-8508 potently inhibits anti-IgM/CD40L-induced proliferation of human B cells, with an IC₅₀ of 0.0064 μM^[1].
AM-8508 potently inhibits anti-IgM-induced AKT phosphorylation in mouse splenic B cells, with an IC₅₀ of 0.0046 μM^[1].
AM-8508 potently inhibits anti-IgD-induced AKT phosphorylation in human whole blood, with a total IC₅₀ of 0.0027 μM and a free IC₅₀ of 1.0 nM^[1].

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

Parmacokinetics

Species	Dose	Route	CL_total	CL_unbound	Bioavailability
Rat^[1]	0.71 mg/kg	i.v.	0.93 L/h/kg	2.6 L/h/kg	/
Rat^[1]	2.0 mg/kg	p.o.	/	/	45 %

In Vivo

AM-8508 (0.03-3 mg/kg; p.o.; single administration) potently inhibits B cell activation-induced AKT phosphorylation in IgM_m mice^[1].
AM-8508 (0.003-0.3 mg/kg, p.o., once daily for 10 consecutive days) dose-dependently suppresses the keyhole limpet hemocyanin (KLH)-induced humoral immune response in female Lewis rats^[1].

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

Animal Model:	IgMₘ transgenic mice^[1]
Dosage:	0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration:	p.o.; single dose
Result:	Showed dose-dependent inhibition of AKT phosphorylation in anti-IgM stimulated B cells isolated from whole blood and spleen compartments. Calculated ED₅₀ values for inhibition of pAKT were <0.03 mg/kg in whole blood and <0.03 mg/kg in splenocytes. Observed statistically significant inhibition relative to the control group at all tested doses.

Animal Model:	Lewis rats (female)^[1]
Dosage:	0.003 mg/kg; 0.01 mg/kg; 0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
Administration:	p.o.; once daily; 10 days
Result:	Inhibited KLH-specific IgG in a dose-dependent manner, with statistically significant inhibition relative to the control group at the 0.1 mg/kg (67% reduction) and 0.3 mg/kg (77% reduction) doses. Showed a dose-dependent reduction in KLH-specific IgM, but this effect was not statistically significant. Calculated ED₅₀ values were 0.08 mg/kg for IgG inhibition and 0.12 mg/kg for IgM inhibition.

Molecular Weight

374.38

Formula

C₁₉H₁₅FN₈

CAS No.

1338483-67-2

SMILES

[C@H](NC=1C(C#N)=C(N)N=CN1)(C)C=2N(C=3C(N2)=CC=C(F)C3)C=4C=CC=NC4

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

Handling Instructions (2659 KB)

References

[1]. Shin Y, et al. Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors. J Med Chem. 2016;59(1):431-447. [Content Brief]

AM-8508 Related Classifications

Inflammation/Immunology

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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:

AM-85081338483-67-2AM8508AM 8508PI3KAktPhosphoinositide 3-kinasePKBProtein kinase BPI3Kδ inhibitorhuman B cellsIgM? transgenic miceLewis ratsInhibitorinhibitorinhibit

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