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Search Results for " pi3k/mtor inhibitor-1 "

21

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12460	PI3K/mTOR Inhibitor-1	PI3K	PI3K/Akt/mTOR signaling
	PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual inhibitor of PI3K/mTOR (PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ/mTOR with IC50s of 20/376/204/46/186 nM)
T6732	WYE-687 N-[4-[4-(4-吗啉基)-1-[1-(3-吡啶甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶-6-基]苯基]氨基甲酸甲酯	p38 MAPK; PI3K; Src; mTOR	Angiogenesis; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	WYE-687 是 ATP 竞争性的 mTOR 抑制剂，其 IC50=7 nM。它能够抑制PI3Kα和PI3Kγ，IC50分别为 81 nM 和 3.11 μM。它能够抑制mTORC1和mTORC2活化。
T2235	Dactolisib 2-甲基-2-[4-[3-甲基-2-氧代-8-(喹啉-3-基)-2,3-二氢咪唑并[4,5-c]喹啉-1-基]苯基]丙腈,BEZ235,NVP-BEZ235	ATM/ATR; PI3K; mTOR; Autophagy	Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	Dactolisib (BEZ235) 是一种可口服的 pan-class IPI3K 和 mTOR 抑制剂，抑制 mTORC1和 mTORC2，作用于 p110α/γ/δ/β和 mTOR，IC50分别为 4 nM/5 nM/7 nM/75 nM 和 20.7 nM。
T1826	PI3K-IN-1 Voxtalisib Analogue,Voxtalisib (SAR245409, XL765) Analogue,XL765,SAR245409	DNA-PK; PI3K	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	PI3K-IN-1 (Voxtalisib Analogue) 是 PI3K 抑制剂，PI3K-IN-1(25 μM) 能够阻断 PI3K/Akt 信号通路。
T36083	DS-7423	PI3K; mTOR	PI3K/Akt/mTOR signaling
	DS-7423 是PI3K 和mTOR 的有效抑制剂，抑制PI3Kα 和 mTOR 的IC50分别为15.6 nM 和 34.9 nM。DS-7423表现出抗癌活性。
T7014	Voxtalisib XL765,SAR245409	DNA-PK; PI3K; mTOR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	Voxtalisib (XL765) 是一种PI3K 抑制剂，抑制p110α，p110β，p110γ和p110δ。它抑制mTORC1和mTORC2，IC50s 分别为 160 和 910 nM。它也抑制 DNA-PK (其 IC50=150 nM) 和 mTOR (其 IC50=157 nM)。
T6045	Torin 1	DNA-PK; PI3K; mTOR; Autophagy	Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	Torin 1 是一种有效的 mTOR 抑制剂，IC50为 3 nM。它抑制 mTORC1/2复合物的 IC50值在 2 和 10 nM 之间，还诱导自噬。
T31223	DCBCI0901 DCBCI-0901,DCBCI 0901
	DCBCI0901 is an inhibitor of phosphatidylinositide 3-kinase (PI3K), raptor-mTOR (mTOR complex 1 or mTORC1) and rictor-mTOR (mTOR complex 2 or mTORC2) with potential antineoplastic activity.
T62438	PI3K/mTOR Inhibitor-9
	PI3K/mTOR Inhibitor-9 (Compound 1) 是一种 mTOR 和 PI3K 的有效抑制剂，能够作用于 mTOR (IC50: 38 nM)、PI3Kα (IC50: 6.6 nM)、PI3Kγ (IC50: 6.6 nM) 和 PI3Kδ (IC50: 0.8 nM)。
T61516	PI3K/mTOR Inhibitor-3
	PI3K/mTOR Inhibitor-3 (compound 12) is an imidazoline compound with potent dual inhibitory effects on PI3K and mTOR. This compound exhibits notable anti-cancer activity [1].
T81470	PI3K/mTOR Inhibitor-14	PI3K	PI3K/Akt/mTOR signaling
	PI3K/mTOR Inhibitor-14（化合物 Y-2）是一种针对PI3K和mTOR的双重抑制剂，其IC50值分别为171.4 nM 和10.1 nM ，具备抗肿瘤活性。
T72374	PI3K/mTOR Inhibitor-12	PI3K	PI3K/Akt/mTOR signaling
	PI3K/mTOR Inhibitor-12为口服有效且选择性的PI3K/mTOR抑制剂，对PI3Kα和mTOR的IC50分别为0.06 nM及3.12 nM，表现出抗肿瘤活性且肝毒性较低。
T36084	PKI-179
	PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo[1][2]. PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1].PKI-179 shows inhibitory activity against a panel of 361 other ...
T62545	HDAC-IN-43
	HDAC-IN-43 是一种强效的 HDAC 1/3/6 抑制剂，对 HDAC 1、HDAC 3 和 HDAC 6 的 IC50 值分别为 82 nM、45 nM 和 24 nM。HDAC-IN-43 是一种弱的 PI3K/mTOR 抑制剂，对 PI3K 和 mTOR 的 IC50 值分别为 3.6 μM 和 3.7 μM。HDAC-IN-43 具有广谱的抗增殖效果。
T63317	ATM Inhibitor-4
	ATM Inhibitor -4 是选择性的、强效的 ATM 抑制剂 (IC50: 0.32 nM)，较强的抑制PI3K 激酶家族的活性，并表现出良好的代谢稳定性。ATM Inhibitor-4 在 1 μM 时能完全抑制mTOR。
T72780	HSP90/mTOR-IN-1
	HSP90/mTOR-IN-1 是一种有效的Hsp90和mTOR 抑制剂，IC50分别为 69 nM 和 29 nM。HSP90/mTOR-IN-1 通过过度激活PI3K/AKT/mTOR 通路抑制 SW780 细胞增殖。HSP90/mTOR-IN-1 通过对HSP90和mTOR 的选择性抑制来诱导细胞凋亡 (apoptosis) 和细胞自噬 (autophagy)。HSP90/mTOR-IN-1 在异种移植小鼠体内也表现出良好的抗肿瘤活性。HSP90/mTOR-IN-1 可用于膀胱癌的研究。
T36314	Wortmannin-Rapamycin Conjugate
	Phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) act synergistically in promoting cancer. Wortmannin is a potent inhibitor of PI3K enzymes, while rapamycin blocks mTOR Complex 1 TORC1. Wortmannin-rapamycin conjugate consists of analogs of 17-hydroxy wortmannin and rapamycin conjugated via a prodrug linker. Hydrolysis of the prodrug linker in vivo releases the inhibitors. The wortmannin-rapamycin conjugate inhibits the growth of HT-29 colon tumors and A498 renal tumors in...
T36308	PF-06843195
	PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy[1]. PF-06843195 inhibits the breast cancer cell lines MCF7 and T47D proliferation with IC50s of 62 nM and 32 nM, respectively[1].PF-06843195 inhibits pAKT (T308) in MCF7 and T47D cells w...
T38263	TBK1/IKKε-IN-4 TBK1/IKKε-IN-4
	TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR[1]. TBK1/IKKε-IN-4 (Compound II; 96 hours; A549 andHCC44 cells) treatmentdisplays selective toxicity in TBK1-dependent cancer cell lines (IC50 of ~ 4.2 μM for H441 cells and IC50 of ~0.4 μM for A549 cells)[1].TBK1/IK...
T6143L	PI-103 Hydrochloride
	PI-103 Hydrochloride 是一种有效的PI3K 和mTOR 双重抑制剂，抑制p110α，p110β，p110δ，p110γ，mTORC1和mTORC2，IC50分别为 8 nM，88 nM，48 nM，150 nM，20 nM 和 83 nM。PI-103 Hydrochloride 也可抑制DNA-PK，IC50为 2 nM。PI-103 Hydrochloride 诱导细胞自噬 (autophagy)。
T82971	ARI-1
	ARI-1是一种针对受体酪氨酸激酶样孤儿受体ROR1的抑制剂，对于ROR1异常表达所致的非小细胞肺癌(NSCLC)及EGFR-TKI诱导的耐药性治疗具有显著效果。该化合物能够特异性结合至ROR1的胞外卷曲结构域，并以ROR1依赖性方式抑制PI3K/AKT/mTOR信号通路，进而有效地阻断NSCLC细胞的增殖和迁移。此外，ARI-1还展现了显著的体内抗肿瘤活性。

化合物

PI3K/mTOR Inhibitor-1

Cat.No: T12460

Target: PI3K

Cat.No: T6732

Synonym: N-[4-[4-(4-吗啉基)-1-[1-(3-吡啶甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶-6-基]苯基]氨基甲酸甲酯

Target: p38 MAPK, PI3K, Src, mTOR

Cat.No: T2235

Synonym: 2-甲基-2-[4-[3-甲基-2-氧代-8-(喹啉-3-基)-2,3-二氢咪唑并[4,5-c]喹啉-1-基]苯基]丙腈,BEZ235,NVP-BEZ235

Target: ATM/ATR, PI3K, mTOR, Autophagy

Cat.No: T1826

Synonym: Voxtalisib Analogue,Voxtalisib (SAR245409, XL765) Analogue,XL765,SAR245409

Target: DNA-PK, PI3K

Cat.No: T36083

Target: PI3K, mTOR

Cat.No: T7014

Synonym: XL765,SAR245409

Target: DNA-PK, PI3K, mTOR

Cat.No: T6045

Target: DNA-PK, PI3K, mTOR, Autophagy

Cat.No: T31223

Synonym: DCBCI-0901,DCBCI 0901

PI3K/mTOR Inhibitor-9

Cat.No: T62438

PI3K/mTOR Inhibitor-3

Cat.No: T61516

PI3K/mTOR Inhibitor-14

Cat.No: T81470

Target: PI3K

PI3K/mTOR Inhibitor-12

Cat.No: T72374

Target: PI3K

Cat.No: T36084

Cat.No: T62545

ATM Inhibitor-4

Cat.No: T63317

HSP90/mTOR-IN-1

Cat.No: T72780

Wortmannin-Rapamycin Conjugate

Cat.No: T36314

Cat.No: T36308

TBK1/IKKε-IN-4

Cat.No: T38263

Synonym: TBK1/IKKε-IN-4

PI-103 Hydrochloride

Cat.No: T6143L

Cat.No: T82971

Cat. No.	Product Name	Target	Signaling Pathways
TN4761	Phellamurin	P-gp	Membrane transporter/Ion channel; Neuroscience
	Phellamurin 是一种来自黄檗叶的黄酮糖苷，可诱导细胞凋亡，具有抗肿瘤活性。它抑制肠道 P-糖蛋白，还抑制凤蝶的产卵。
T2P2806	Hederacolchiside A1 黑海常春藤苷A1,革叶常春藤皂苷 A1,Raddeanoside R13	Apoptosis; ERK; MEK; Akt; PI3K; Parasite; mTOR	Apoptosis; Cytoskeletal Signaling; MAPK; Microbiology/Virology; PI3K/Akt/mTOR signaling
	Hederacolchiside A1 (Raddeanoside R13) 是从白头翁中分离的一种有抗利什曼原虫和抗肿瘤增殖活性的天然产物。

天然产物

Cat.No: TN4761

Target: P-gp

Hederacolchiside A1

Cat.No: T2P2806

Synonym: 黑海常春藤苷A1,革叶常春藤皂苷 A1,Raddeanoside R13

Target: Apoptosis, ERK, MEK, Akt, PI3K, Parasite, mTOR

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