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.
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- CAS No.: 2125500-60-7
- 화학식: C26H26F2N6O5S
- 분자량:572.58
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
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
-
분자량 572.58
-
화학식 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
-
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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)