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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2125500-60-7
- 分子式: C26H26F2N6O5S
- 分子量:572.58
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
|
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] |
化学情報
-
CAS 番号 2125500-60-7
-
分子量 572.58
-
分子式 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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)