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27

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7506	Yoda 1	Piezo Channel	Membrane transporter/Ion channel
	Yoda 1 是Piezo1激动剂，能够激活纯化的 Piezo1 通道。
T8151	Mobocertinib tak788	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Mobocertinib (tak788) 是可口服的EGFR 和HER2突变的抑制剂，具有抗肿瘤活性。
T6928	Pantoprazole SKF96022,泮托拉唑,BY1023	Apoptosis; Proton pump; Autophagy	Apoptosis; Autophagy; Membrane transporter/Ion channel
	Pantoprazole (BY1023) 是一种质子泵抑制剂，用于短期治疗由胃食管反流病引起的食管糜烂和溃疡。它联合阿霉素可显著增加肿瘤生长延迟。它是一种取代的苯并咪唑，是H+/K+-ATPase 抑制剂，可改善 pH 值稳定性，具有抗分泌和抗溃疡的作用。
T2325	Neratinib HKI-272,来那替尼	EGFR; HER	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Neratinib (HKI-272) 是一种口服的、不可逆的酪氨酸激酶抑制剂，对 HER2 和 EGFR 的 IC50值分别为 59 和 92 nM。
T21312	Afatinib 阿法替尼,Afatinib free base,BIBW 2992	EGFR; Autophagy	Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Afatinib (BIBW 2992) 是一种不可逆的 EGFR 家族抑制剂，抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。
T2586	Cabozantinib 卡博替尼,XL184,BMS-907351	Apoptosis; VEGFR; FLT; c-Met/HGFR; c-RET; TAM Receptor; c-Kit	Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors
	Cabozantinib (XL184) 是一种多靶点酪氨酸激酶受体抑制剂，可以抑制 VEGFR2、c-Met、Kit、Axl 和 Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM)。Cabozantinib 具有抗肿瘤和抗血管生成活性。
T0161	Pantoprazole Sodium Hydrate SKF96022 sodium hydrate,泮托拉唑钠水合物,BY1023 (sodium hydrate),SKF96022 (sodium hydrate)	Apoptosis; Potassium Channel; Proton pump; Autophagy	Apoptosis; Autophagy; Membrane transporter/Ion channel
	Pantoprazole Sodium Hydrate (BY1023 (sodium hydrate)) 是一种具有口服活性的质子泵抑制剂。它是取代的苯并咪唑，是H+/K+-ATPase 抑制剂。它可改善 pH 值稳定性，具有抗分泌和抗溃疡的作用。它联合阿霉素可显著增加肿瘤生长延迟。
T5164	Cabozantinib hydrochloride XL184,Cabozantinib hydrochloride (849217-68-1(free base)),BMS-907351,盐酸卡博替尼	VEGFR; FLT; c-Met/HGFR; TAM Receptor; c-Kit; ROR	Angiogenesis; Metabolism; Tyrosine Kinase/Adaptors
	Cabozantinib hydrochloride (XL184) 是一种有效的泛酪氨酸激酶抑制剂，可抑制 VEGFR2、c-Met、Kit、Axl 和 Flt4（IC50：0.035、1.3、4.6、7 和 6 nM）。
T6929	Pantoprazole sodium Pantecta,泮托拉唑钠盐,SKF96022 sodium,SKF96022 (sodium),BY1023 (sodium),泮托拉唑钠,BY-1023 sodium,Pantoloc	Apoptosis; Others; Proton pump; HIF; Autophagy	Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; Membrane transporter/Ion channel; Others
	Pantoprazole sodium (Pantecta) 是一种具有口服活性的质子泵抑制剂，是一种取代的苯并咪唑，是H+/K+-ATPase 抑制剂，IC50为 6.8 μM。它可以改善 pH 值稳定性，具有抗分泌和抗溃疡的作用。它联合阿霉素可显著增加肿瘤生长延迟。
T1773	Afatinib Dimaleate 马来酸阿法替尼,双马来酸盐阿法替尼,BIBW2992,Afatinib,BIBW 2992MA2,Afatinib (BIBW2992) Dimaleate	EGFR; HER; Autophagy	Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Afatinib Dimaleate (BIBW 2992MA2) 是一种可口服的苯胺基-喹唑啉衍生物和受体酪氨酸激酶表皮生长因子受体家族的抑制剂，具有抗肿瘤活性。它抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。
T77718	FAK-IN-10	FAK	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	FAK-IN-10 是一种 FAK 的抑制剂（IC50:76.3 μM)。FAK-IN-10 z MCF-7 和 A431 细胞系中显示出抗肿瘤活性，IC50 分别为 4.23 和 0.78 μM 。
T5155	(E)-AG 99 (E)-Tyrphostin AG 99,(E)-Tyrphostin 46,AG 99,Tyrphostin 46	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	(E)-AG 99 ((E)-Tyrphostin AG 99) 是一种 EGFR 抑制剂。
T64124	Sunvozertinib DZD9008,DZD 9008,DZD-9008	EGFR; BTK	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Sunvozertinib (DZD9008) 是一种有效的 ErbBs 和 BTK 抑制剂，对EGFR、Her2和突变型表皮生长因子有抑制作用。 Sunvozertinib 显示 EGFR 外显子 20 NPH 插入、EGFR 外显子 20 ASV 插入、EGFR L858R 和 T790M 突变以及 Her2 外显子 20 YVMA 和 EGFR WT A431 有抑制作用， IC50 分别为 20.4、20.4、1.1、7.5 和 80.4 nM 。
T8525	EGFR-IN-16 AG473	EGFR; FGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	EGFR-IN-16 (AG473) 是一种EGFR 抑制剂，对 EGFR 和 HER-2 的pIC50分别为4.85和4.74。
T60314	Anticancer agent 38
	Anticancer agent 38 (compound 19) 是芳基脲化合物，是一种有效的抗癌剂。Anticancer agent 38 抑制 A431 细胞生长的 IC50为 5.2 μg/mL。
T79888	EGFR-IN-87	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	EGFR-IN-87 为EGFR酪氨酸激酶抑制剂，针对A431细胞中EGFR_d746-750, EGFR_L858R/T790M 及 EGFR_WT 具有IC50值分别约为3.1 nM、1.3 nM和7.1 nM，适用于癌症疾病研究。
T73101	EGFR-IN-25
	EGFR-IN-25 是一种有效的EGFR 抑制剂，对 BaF3 细胞 (EGFR DEL19/T790M/C797S) 和 A431 细胞 (WT) 的IC50分别为 9 nM 和 60 nM。
T9905	Cetuximab Cetuximab (anti-EGFR),C225,西妥昔单抗	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Cetuximab (C225) 属于单克隆抗体，是一种人源表皮生长因子受体 (EGFR) 的抑制剂 (Kd=0.201 nM)。Cetuximab 具有抗肿瘤活性，可以抑制肿瘤细胞增殖，诱导细胞凋亡。
T61602	Anticancer agent 35
	Anticancer agent 35 (compound 10) 是一种磺酰脲类衍生物，一种有效的抗癌剂。Anticancer agent 35 抑制 A549、A431、PACA2 细胞生长，IC50分别为 18.1 μg/mL、4.0 μg/mL、18.9 μg/mL。
T61827	RJ-34
	RJ-34, an aristolactam analogue, demonstrates strong antitumor effects across a wide range of cancer cell lines, with subnanomolar GI 50 values (GI 50 <0.1 nM) observed for A431, MES-SA, MES-SA/DX5, HCT-15, and HCT-15/CLO2 cells [1].
T37586	DMHAPC-Chol
	DMHAPC-Chol is a cationic cholesterol. Liposomes containing DMHAPC-chol have been used for DNA plasmid delivery in vitro and in vivo in a B16-F10 mouse xenograft model. Liposomes containing DMHAPC-chol are cytotoxic to B16-F10 cells when used at lipid concentrations greater than 20 μM. DMHAPC-Chol, as part of a lipoplex with DOPE , has also been used to deliver DNA into mouse lung via intratracheal injection, resulting in a heterogeneous distribution in the bronchi and bronchioles, and to delive...
T69438	MT477
	MT477 is PKC-α inhibitor. MT477 interfered with PKC activity as well as phosphorylation of Ras and ERK1/2 in H226 human lung carcinoma cells. It also induced poly-caspase-dependent apoptosis. MT477 had a dose-dependent (0.006 to 0.2 mM) inhibitory effect on cellular proliferation of H226, MCF-7, U87, LNCaP, A431 and A549 cancer cell lines as determined by in vitro proliferation assays.
T63769	EGFR-IN-60
	EGFR-IN-60 是一种有效的、口服具有活力的、安全的抗肿瘤剂。EGFR-IN-60 能够明显抑制 EGFRWT (IC50: 83 nM)、EGFRT790M (IC50: 26 nM)、EGFRL858R (IC50: 53 nM) 和 JAK3 (IC50: 69 nM)。EGFR-IN-60 能够抑制携带 EGFRT790M 突变的 H1975 细胞 (IC50: 1.32 μM) ，并抑制过表达 EGFRWT 的 A431 细胞 (IC50: 4.96 μM)。EGFR-IN-60 能够提高 Bax/Bcl-2 比率，进而诱导细胞凋亡诱导并导致细胞死亡。
T35671	Salazinic Acid
	Salazinic acid is a depsidone lichen metabolite that has been found in P. sulcata.1 It is active against B. cereus, B. subtilis, S. aureus, P. aeruginosa, S. typhimurium, C. albicans, and A. niger in vitro (MICs = 3.9-30.8 mM). Salazinic acid is cytotoxic to MM98, A431, and HaCaT cells in crystal violet (EC50s = 159, 2,870, and 48 μM, respectively) and neutral red uptake assays (EC50s = 1,925, 1,913, and 907 μM, respectively).2 It increases the wound closure rate in scratch-wounded HaCaT monolay...
T36844	Inostamycin A
	Inostamycin A is a bacterial metabolite that has been found inStreptomycesand has anticancer activity.1It is an inhibitor of CDP-diacylglycerol:inositol 3-phosphatidyltransferase (IC50= 0.02 μg/ml in A431 cell membranes) and is selective for CDP-diacylglycerol:inositol 3-phosphatidyltransferase over phospholipase C (PLC) and phosphatidylinositol kinase at 10 μg/ml.2Inostamycin A decreases viability of YCU-T892, KCC-TC873, KB, HSC-4, and YCU-T891 oral squamous cell carcinoma (OSCC) cells in a con...
T36907	1-Oleoyl Lysophosphatidic Acid Oleoyl-sn-3-Glycerophosphate,1-Oleoyl LPA,1-Oleoyl Lysophosphatidic Acid
	1-Oleoyl lysophosphatidic acid is a species of lysophosphatidic acid (LPA) containing oleic acid at the sn-1 position. Phosphatidic acid is produced either directly through the action of phospholipase D (PLD) or through a two step process involving liberation of diacylglycerol (DAG) by phospholipase C (PLC) followed by phosphorylation of DAG by diglycerol kinase.[1] Hydrolysis of the fatty acid at the sn-2 position by phospholipase A2 (PLA2) yields bioactive LPA. LPA binds to one of five differe...
T35897	ASK120067
	ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT...

化合物

Cat.No: T7506

Target: Piezo Channel

Cat.No: T8151

Synonym: tak788

Target: EGFR

Cat.No: T6928

Synonym: SKF96022,泮托拉唑,BY1023

Target: Apoptosis, Proton pump, Autophagy

Cat.No: T2325

Synonym: HKI-272,来那替尼

Target: EGFR, HER

Cat.No: T21312

Synonym: 阿法替尼,Afatinib free base,BIBW 2992

Target: EGFR, Autophagy

Cat.No: T2586

Synonym: 卡博替尼,XL184,BMS-907351

Target: Apoptosis, VEGFR, FLT, c-Met/HGFR, c-RET, TAM Receptor, c-Kit

Pantoprazole Sodium Hydrate

Cat.No: T0161

Synonym: SKF96022 sodium hydrate,泮托拉唑钠水合物,BY1023 (sodium hydrate),SKF96022 (sodium hydrate)

Target: Apoptosis, Potassium Channel, Proton pump, Autophagy

Cabozantinib hydrochloride

Cat.No: T5164

Synonym: XL184,Cabozantinib hydrochloride (849217-68-1(free base)),BMS-907351,盐酸卡博替尼

Target: VEGFR, FLT, c-Met/HGFR, TAM Receptor, c-Kit, ROR

Pantoprazole sodium

Cat.No: T6929

Synonym: Pantecta,泮托拉唑钠盐,SKF96022 sodium,SKF96022 (sodium),BY1023 (sodium),泮托拉唑钠,BY-1023 sodium,Pantoloc

Target: Apoptosis, Others, Proton pump, HIF, Autophagy

Afatinib Dimaleate

Cat.No: T1773

Synonym: 马来酸阿法替尼,双马来酸盐阿法替尼,BIBW2992,Afatinib,BIBW 2992MA2,Afatinib (BIBW2992) Dimaleate

Target: EGFR, HER, Autophagy

Cat.No: T77718

Target: FAK

Cat.No: T5155

Synonym: (E)-Tyrphostin AG 99,(E)-Tyrphostin 46,AG 99,Tyrphostin 46

Target: EGFR

Cat.No: T64124

Synonym: DZD9008,DZD 9008,DZD-9008

Target: EGFR, BTK

Cat.No: T8525

Synonym: AG473

Target: EGFR, FGFR

Anticancer agent 38

Cat.No: T60314

Cat.No: T79888

Target: EGFR

Cat.No: T73101

Cat.No: T9905

Synonym: Cetuximab (anti-EGFR),C225,西妥昔单抗

Target: EGFR

Anticancer agent 35

Cat.No: T61602

Cat.No: T61827

Cat.No: T37586

Cat.No: T69438

Cat.No: T63769

Cat.No: T35671

Cat.No: T36844

1-Oleoyl Lysophosphatidic Acid

Cat.No: T36907

Synonym: Oleoyl-sn-3-Glycerophosphate,1-Oleoyl LPA,1-Oleoyl Lysophosphatidic Acid

Cat.No: T35897

Cat. No.	Product Name	Target	Signaling Pathways
TN6569	cis-Moschamine
	cis-Moschamine exerts antitumour effects on HeLa, MCF7 and A431 cells.
T2S0961	Chalcone benzylideneacetophenone,phenyl styryl ketone,Cinnamophenone,benzalacetophenone,β-phenylacrylophenone,查耳酮	EGFR; Antibacterial	Angiogenesis; JAK/STAT signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors
	Chalcone (Cinnamophenone) 是从甘草中分离得到的一种芳香酮，可合成查耳酮衍生物。它具有多种生物和药理的活性，如抗炎、抗菌、抗癌、抗氧化、抗寄生虫等活性。

天然产物

Cat.No: TN6569

Cat.No: T2S0961

Synonym: benzylideneacetophenone,phenyl styryl ketone,Cinnamophenone,benzalacetophenone,β-phenylacrylophenone,查耳酮

Target: EGFR, Antibacterial

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