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Cat. No.: HY-164384

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DFX117

DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC₅₀s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice.

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

CAS No.: 2125500-60-7
Formula: C₂₆H₂₆F₂N₆O₅S
Molecular Weight:572.58

Storage:

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

Data Sheet (271 KB)

DFX117 Chemical Structure

CAS No.: 2125500-60-7

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

All PI3K Isoforms :

All Akt Isoforms :

All mTOR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.04 μM Compound: 1i	Antiproliferative activity against human A549 cells after 72 hrs by SRB assay Antiproliferative activity against human A549 cells after 72 hrs by SRB assay	[PMID: 28800461]
A549	IC₅₀	0.04 μM Compound: 76	Antiproliferative activity against human A549 cells by MTT assay Antiproliferative activity against human A549 cells by MTT assay	[PMID: 38733884]
HCC827	IC₅₀	0.08 μM Compound: 76	Antiproliferative activity against human HCC827 cells by MTT assay Antiproliferative activity against human HCC827 cells by MTT assay	[PMID: 38733884]
HCT-116	IC₅₀	0.01 μM Compound: 1i	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 28800461]
HCT-116	IC₅₀	0.34 μM Compound: 1i	Cytotoxicity against human HCT116 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human HCT116 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 32069401]
HUVEC	IC₅₀	2.94 μM Compound: 1i	Cytotoxicity against against HUVEC after 72 hrs by SRB assay Cytotoxicity against against HUVEC after 72 hrs by SRB assay	[PMID: 28800461]
MDA-MB-231	IC₅₀	0.04 μM Compound: 1i	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay	[PMID: 28800461]
NCI-H1975	IC₅₀	0.02 μM Compound: 76	Antiproliferative activity against human NCI-H1975 cells by MTT assay Antiproliferative activity against human NCI-H1975 cells by MTT assay	[PMID: 38733884]
NCI-H1993	IC₅₀	0.05 μM Compound: 76	Antiproliferative activity against human NCI-H1993 cells by MTT assay Antiproliferative activity against human NCI-H1993 cells by MTT assay	[PMID: 38733884]
SK-HEP1	IC₅₀	0.11 μM Compound: 1i	Antiproliferative activity against human SKHEP1 cells after 72 hrs by SRB assay Antiproliferative activity against human SKHEP1 cells after 72 hrs by SRB assay	[PMID: 28800461]
SNU-638	IC₅₀	0.01 μM Compound: 1i	Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay	[PMID: 28800461]

Chemical Information

CAS No. 2125500-60-7
Molecular Weight 572.58
Formula C₂₆H₂₆F₂N₆O₅S
SMILES

O=C(C1=CN=C2C=CC(C3=CC(NS(=O)(C4=CC=C(C=C4F)F)=O)=C(OC)N=C3)=CN21)NCCN5CCOCC5
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 (271 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]. Fan Y, et al., Antitumor Activity of DFX117 by Dual Inhibition of c-Met and PI3Kα in Non-Small Cell Lung Cancer. Cancers (Basel). 2019 May 5;11(5):627. [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.

Keywords

100 mg

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Biological Activity
- Description
Chemical Information
Purity & Documentation
References

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DFX117

All PI3K Isoforms

All Akt Isoforms

All mTOR Isoforms