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Cat. No.: HY-150638

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PI3Kδ/γ-IN-3

PI3Kδ/γ-IN-3 (Compound 58) is a potent and orally active PI3Kδ and PI3Kγ dual inhibitor with IC₅₀s of 1 nM and 16 nM, respectively. PI3Kδ/γ-IN-3 induces tumor cell apoptosis and can be used for B-cell malignancies research.

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

CAS No.: 2730151-31-0
Formula: C₂₃H₂₀ClN₉O
Molecular Weight:473.92

Storage:

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

Data Sheet (287 KB)

PI3Kδ/γ-IN-3 Chemical Structure

CAS No.: 2730151-31-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

PI3Kδ

1 nM (IC₅₀)

PI3Kγ

16 nM (IC₅₀)

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
DOHH-2	IC₅₀	0.2 μM Compound: 58	Antiproliferative activity against human DOHH-2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human DOHH-2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 35831917]
SUD4	IC₅₀	0.03 μM Compound: 58	Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 35831917]
SU-DHL-6	IC₅₀	0.06 nM Compound: 58	Antiproliferative activity against human SUDHL2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human SUDHL2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 35831917]
SU-DHL-6	IC₅₀	0.06 μM Compound: 58	Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 35831917]

In Vitro

PI3Kδ/γ-IN-3 (Compound 58) (72 h) shows antiproliferative activity against B-cell lymphoma (DLBCL) cells^[1].
PI3Kδ/γ-IN-3 (0.5 μM, 24 h) arrests cell cycle at G0/G1 phase in SUDHL-6 and DOHH2 cells^[1].
PI3Kδ/γ-IN-3 (1.5 and 2 μM, 48 h) induces cell apoptosis in SUDHL-6 and DOHH2 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

SUDHL-4, SUDHL-6 and DOHH2 cells
Concentration:
Incubation Time:

72 h
Result:

Showed antiproliferative activity with IC₅₀s of 0.03 ± 0.03, 0.06 ± 0.01 and 0.20 ± 0.04 μM against SUDHL-4, SUDHL-6 and DOHH2 cells, respectively.

Cell Cycle Analysis^[1]

Cell Line:

SUDHL-6 and DOHH2 cells
Concentration:

0.5 μM
Incubation Time:

Alone or in combination with Ibrutininb (HY-10997) (0.5 μM or 1 μM) for 24 h
Result:

Caused a loss of G2/M phase cells and an increase in the percentage of cells in the G0/G1 phase. Induced cell cycle arrest alone or in combination with Ibrutinib in both cells.

Apoptosis Analysis^[1]

Cell Line:

SUDHL-6 and DOHH2 cells
Concentration:

1.5 μM and 2 μM
Incubation Time:

Alone or in combination with Ibrutininb (1.5 μM or 1 μM) for 48 h
Result:

Demonstrated the induction of apoptosis in both SUDHL-6 and DOHH2 cells, and the combination was stronger than treated alone.

In Vivo

PI3Kδ/γ-IN-3 (Compound 58) (5 and 10 mg/kg; p.o.; daily for 14d) suppresses the tumor volume in a dose-dependent manner without obvious toxicity in mice^[1].

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

Animal Model:

Female non obese diabetes/severe combined immunodeficient (NOD/SCID) mice, 6- to 8-week-old, SUDHL-6 xenograft model^[1]
Dosage:

5 and 10 mg/kg alone or in combination with 10 mg/kg Ibrutinib
Administration:

Oral administration, daily for 14 days
Result:

Suppressed the tumor volume in a dose-dependent manner and demonstrated superior efficacy relative to Ibrutinib at 10 mg/kg QD administration. When in combination with Ibrutinib, showed greater tumor growth inhibitory effects.

Animal Model:

SD rats^[1]
Dosage:

5 mg/kg
Administration:

Oral or intravenous administration (Pharmacokinetic Analysis)

Result:

PK Profiles of PI3Kδ/γ-IN-3 (Compound 58) in Male SD Rats^[1]

Compound	dose (mg/kg)	administration route	C_max (ng/mL)	T_max (h)	AUC_0-t (h•μg/L)	T_1/2 (h)	CL (L/h/kg)	V_ss(L/kg)	F (%)
58	5	oral	3637.81	3.33	8612.57	9.46	0.79	--	126.5
	5	intravenous	860.09	0.08	6806.92	2.79	0.75	2.86	--

PK profiles: C_max, maximum plasma concentration; T_max, tim

Chemical Information

CAS No. 2730151-31-0
Molecular Weight 473.92
Formula C₂₃H₂₀ClN₉O
SMILES

O=C1N(C2=CN=CC=C2)C([C@H]3N(C4=NC(N)=NC(N)=C4C#N)[C@H](CC3)C)=NC5=CC=CC(Cl)=C51
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Liu K, et al. Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies. J Med Chem. 2022 Jul 13. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PI3Kδ/γ-IN-3

All PI3K Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PI3Kδ/γ-IN-3 Related Classifications

HY-150638 Related Classifications