2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Akt mTOR Apoptosis
  4. DFX117

DFX117 是口服有效的 PI3Kα 和 c-Met 酪氨酸激酶 (c-Met) 选择性抑制剂。DFX117 抑制 PI3K/Akt/mTOR 通路，抑制 NCI-H1975、NCI-H1993 和 HCC827 的增殖，IC50 为 0.02-0.08 µM。DFX117 在 G0/G1 期阻滞细胞周期，诱导 A549 和 NCI-H1975 细胞凋亡 (apoptosis)。DFX117 在小鼠中表现出抗肿瘤活性。i

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DFX117

DFX117 Chemical Structure

CAS No. : 2125500-60-7

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DFX117 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

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mTOR mTORC1 mTORC2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

细胞效力
(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]
分子量

572.58

Formula

C26H26F2N6O5S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DFX117 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DFX1172125500-60-7DFX 117DFX-117PI3KAktmTORApoptosisPhosphoinositide 3-kinasePKBProtein kinase BMammalian target of RapamycinNCI-H1975NCI-H1993HCC827selectiveA549orally activeICR mouseInhibitorinhibitorinhibit

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