Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1921 |
Alpelisib
BYL-719 |
PI3K | PI3K/Akt/mTOR signaling |
Alpelisib (BYL-719) 是一种 PI3Kα 抑制剂 (IC50=5 nM),具有选择性、有效性和口服活性。Alpelisib 以较低活性抑制 PI3Kβ/γ/δ (IC50=250/290/1200 nM)。Alpelisib 具有抗肿瘤活性,对 PIK3CA 突变肿瘤具有靶向性。 | |||
T1952 |
MK-2206 dihydrochloride
MK-2206 2HCl |
Apoptosis; Akt; Autophagy | Apoptosis; Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
MK-2206 dihydrochloride (MK-2206 2HCl) 是一种变构 Akt 抑制剂,抑制 Akt1、Akt2 和 Akt3 (IC50=8/12/65 nM),具有口服活性的、高效选择性。MK-2206 dihydrochloride 具有抗肿瘤活性。 | |||
T14511 |
BAY1082439
N-[8-[[(2R)-2-羟基-3-(吗啉-4-基)丙基]氧基]-7-甲氧基-2,3-二氢咪唑并[1,2-C]喹唑啉-5-基]-2-甲基吡啶-3-甲酰胺 |
Apoptosis; PI3K | Apoptosis; PI3K/Akt/mTOR signaling |
BAY1082439 是一种具有口服活性的,选择性 PI3Kα/β/δ抑制剂。它也能抑制 PIK3CA 的突变形式,它对抑制 Pten 丢失的前列腺癌的生长有很强的作用。 | |||
T67703 |
mTOR inhibitor 9b
|
mTOR | PI3K/Akt/mTOR signaling |
mTOR inhibitor 9b 是一种酶抑制剂,对蛋白激酶mTOR 和磷脂酰肌醇 3-激酶 PIK3CA 具有抑制作用,IC50分别为 0.76nm 和1.262 µM。mTOR inhibitor 9b 具有抗癌活性,可用来研究白血病、皮肤癌、乳腺癌、肺癌和结肠癌。 | |||
T1999 |
Taselisib
RG-7604,GDC-0032 |
PI3K; Carbonic Anhydrase | Metabolism; PI3K/Akt/mTOR signaling |
Taselisib (GDC-0032) 是 PI3K 抑制剂,靶向作用于突变 PI3KCA。它能够抑制 PI3Kα (IC50:0.29 nM),PI3Kβ (IC50:0.91 nM) 和 PI3Kγ (IC50:0.97 nM)。 | |||
T35343 |
MTI-31
MTI-31,LXI-15029 |
mTOR | PI3K/Akt/mTOR signaling |
MTI-31 (LXI-15029) 是口服有效的,高度选择性的mTORC1和mTORC2抑制剂,对 mTOR 的Kd 为 0.20 nM,IC50为 39 nM。MTI-31可用于乳腺癌的研究。 | |||
T67705 |
mTOR inhibitor 9a
|
||
mTOR inhibitor 9a 对人LNCap 细胞的生长具有抑制作用,ic50为80nm。mTOR inhibitor 9a 可能具有抗肿瘤活性。 | |||
T71197 | JW-7-25-1 | ||
JW-7-25-1 is a potent multi-target inhibitor, acting on MELK, PIK3CA, mTOR, GSK3A and CDK7. | |||
T27621 |
Ipatasertib HCl
GDC0068,RG 7440,GDC 0068,RG-7440,GDC-0068,RG7440 |
||
Ipatasertib is an orally active, potent and selective Akt inhibitor with antitumor activity. Inhibition of Akt activity by Ipatasertib resulted in blockade of cell-cycle progression and reduced viability of cancer cell lines. Markers of Akt activation, in | |||
T81784 |
MK-2206 free base
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
MK-2206 free base是一种口服活性、高选择性的变构Akt抑制剂,IC50分别针对Akt1、Akt2、Akt3为8、12和65 nM 。多种乳腺癌细胞系、PIK3CA突变以及PTEN缺失细胞系对此化合物敏感,显示出抗癌活性。 | |||
T62609 |
MK-2206
|
||
MK-2206 是一种具有口服具有活力的、高效选择性的变构 Akt 抑制剂,能够作用于 Akt1 (IC50: 8 nM)、Akt2 (IC50: 12 nM) 和 Akt3 (IC50: 65 nM)。许多乳腺癌细胞系、PIK3CA 突变体和 PTEN 丢失细胞系对 MK-2206 敏感。MK-2206 具有抗癌作用。 | |||
T67702 |
mTOR inhibitor 9d
|
PI3K; mTOR | PI3K/Akt/mTOR signaling |
mTOR inhibitor 9d 是一种蛋白激酶 mTOR 和PI3K 双重抑制剂,对mTOR 的IC50值为0.31nm,可用于治疗白血病、皮肤癌、乳腺癌、肺癌和结肠癌。 | |||
T38847 |
Vevorisertib
Vevorisertib,ARQ 751 |
||
Vevorisertib (ARQ 751) is a highly effective oral compound that selectively inhibits pan-AKT serine/threonine kinases such as AKT1 (with an IC50 value of 0.55 nM), AKT2 (with an IC50 value of 0.81 nM), and AKT3 (with an IC50 value of 1.31 nM). This compound, either as a standalone treatment option or in combination with other anti-cancer agents, is ideally suited for conducting research on solid tumors characterized by PIK3CA/AKT/PTEN mutations[4]. | |||
T70552 |
Ipatasertib tosylate
|
||
Ipatasertib, also known as GDC0068, is an orally active, potent and selective Akt inhibitor. GDC-0068 blocked Akt signaling both in cultured human cancer cell lines and in tumor xenograft models. Inhibition of Akt activity by GDC-0068 resulted in blockade of cell-cycle progression and reduced viability of cancer cell lines. Markers of Akt activation, including high-basal phospho-Akt levels, PTEN loss, and PIK3CA kinase domain mutations, correlate with sensitivity to GDC-0068. In multiple tumor... | |||
TP2288 |
Rapalink-1
|
Others | Others |
RapaLink-1 is the third-generation mTOR inhibitor exploiting the unique juxtaposition of two drugs (first- and second-generation mTOR kinase inhibitors) -binding pockets to create a bivalent interaction that allows inhibition of the mutants which has resi | |||
T72071 | WAY-299017 | Antibacterial | Microbiology/Virology |
WAY-299017是一种强效且具有选择性的UPPS 抑制剂,可用于治疗细菌感染。 |