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Cat. No.: HY-128633

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DHW-208

PI3K-IN-4 is a potent Pan-PI3K inhibitor. PI3K-IN-4 has high activity for three PI3K isoforms with the IC₅₀ values of picomole. PI3K-IN-4 shows superior inhibitory activity against PI3Kα (IC₅₀ = 0.20 nM), PI3Kβ (IC₅₀ = 2.99 nM), PI3Kδ (IC₅₀ = 0.48 nM) and PI3Kγ (IC₅₀ = 0.58 nM) and has no significant activity against EGFR. PI3K-IN-4 inhibits cancer cell growth though PI3K/Akt signaling pathway, leading to the inhibition of colony formation and the induction of apoptosis. PI3K-IN-4 can be used for lung, colon and breast cancer research.

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CAS No.: 2269470-35-9
화학식: C₂₅H₂₁F₂N₇O₄S
분자량:553.54

보관:

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

Data Sheet (280 KB)

DHW-208 Chemical Structure

CAS No.: 2269470-35-9

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

PI3Kα

0.20 nM (IC₅₀)

PI3Kβ

2.99 nM (IC₅₀)

PI3Kγ

0.58 nM (IC₅₀)

PI3Kδ

0.48 nM (IC₅₀)

All PI3K Isoforms :

All Akt Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	3.1 μM Compound: 7b	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31097403]
HCT-116	IC₅₀	0.33 μM Compound: 7b	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31097403]
HUVEC	IC₅₀	19.6 μM Compound: 7b	Cytotoxicity against HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31097403]
L02	IC₅₀	60 μM Compound: 7b	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31097403]
MCF7	IC₅₀	0.22 μM Compound: 7b	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31097403]

In Vitro

PI3K-IN-4 (compound 7b) (72h) shows antiproliferation activity against typically human cancer cells with IC₅₀ values of 3.10 μM (A549), 0.33 μM (HCT116), and 0.22 μM (MCF-7), and displays much lower cytotoxicity in HUVEC (IC₅₀ = 19.6 μM) and HL7702 normal cells (IC₅₀ = 60.0 μM)^[1].
PI3K-IN-4 (0.1-10 μM) decreases the phospho-Akt (S473) in a dose-dependent manner and down-regulated p-Akt/Akt ratio in MCF-7 cells, suggesting it might inhibit MCF-7 cell growth though PI3K/Akt signaling pathway^[1].
PI3K-IN-4 (0.2-0.8 μM, 72 h) inhibits colony formation and inhibit the proliferation of MCF-7 cells in a dose-dependent manner^[1].
PI3K-IN-4 (0.2-0.8 μM, 48 h) induces apoptosis in MCF-7 cells with markable nuclear fragmentation and condensation of chromatin^[1].
PI3K-IN-4 forms four key hydrogen bonds with PI3K, one more than Omipalisib (HY-10297), which may contribute to its superior binding stability and activity^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

MCF-7 cells
Concentration:

0.2, 0.4 and 0.8 μM
Incubation Time:

72 h
Result:

Inhibited the cell proliferation in a dose-dependent manner.
Significantly inhibit colony formation at a concentration of 0.8 μM.

Apoptosis Analysis^[1]

Cell Line:

MCF-7 cells
Concentration:

0.2, 0.4 and 0.8 μM
Incubation Time:

48 h
Result:

Induced cell apoptosis with the highest apoptosis percentage of 27.5 % at 0.8 μM.
Resulted in nuclear fragmentation and condensation of chromatin.

Chemical Information

CAS No. 2269470-35-9
분자량 553.54
화학식 C₂₅H₂₁F₂N₇O₄S
SMILES

COC(N=C1)=C(NS(=O)(C2=CC=C(F)C=C2F)=O)C=C1C3=CC=C(N=CN=C4NC5=CN(CCO)N=C5)C4=C3
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 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]. Ding HW, et al. Design, synthesis, and biological evaluation of some novel 4-aminoquinazolines as Pan-PI3K inhibitors. Bioorg Med Chem. 2019 Jul 1;27(13):2729-2740. [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

DHW-208

All PI3K Isoforms

All Akt Isoforms