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23

抑制剂 & 化合物

4

天然产物

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Cat. No. Product Name Target Signaling Pathways
T17731L CL2A-SN-38 DCA 1279680-68-0(free base)

Others Others
CL2A-SN-38 DCA 1279680-68-0(free base) 是一种药物-接头偶联物,由有效的 DNA 拓扑异构酶 I 抑制剂 SN-38 和接头 CL2A 组成,用于制造抗体药物偶联物 (ADC)。CL2A-SN-38 由有效的 DNA 拓扑异构酶组成I 抑制剂 SN-38 和接头 CL2A 以制造抗体药物偶联物 (ADC)。 CL2A-SN-38 对一系列人类实体瘤类型提供显着和特异性的抗肿瘤作用。 CL2A 是一种不可切割的复杂 PEG8 和含有三唑的 PABC-肽-mc 接头。 CL2A 可通过 pH 敏感性裂解,产生旁观者效应,并通过二硫键在半胱氨酸残基处结合抗体。
T39222 Mc-VC-PAB-SN38

Mc-VC-PAB-SN38

Others Others
Mc-VC-PAB-SN38 由可降解 (cleavable) 的 ADC linker (Mc-VC-PAB) 和 SN38 组成,属于抗体偶联活性分子的一部分,常用来合成靶向作用位点的抗体偶联活性分子 (ADC)。
T17731 CL2A-SN-38

Others Others
CL2A-SN-38 是一种药物-接头偶联物,由一种有效的 DNA 拓扑异构酶 I 抑制剂 SN-38 和接头 CL2A 组成,用于制造抗体药物偶联物。它对一系列人类实体瘤类型提供显着和特异性的抗肿瘤作用。
T10832 CL2-SN-38

Others Others
CL2-SN-38, a part of the antibody-drug conjugate (ADC), can conjugate with the anti-Trop-2-humanized antibody hRS7. SN-38 is an inhibitor of DNA topoisomerase I.
T38962 MC-SN38

MC-SN38

MC-SN38 is a drug-linker conjugate that pairs the potent microtubule-disrupting agent SN38 with a non-cleavable MC linker, designed for use in antibody drug conjugates (ADCs). SN38, the active metabolite of the Topoisomerase I inhibitor Irinotecan, works by inhibiting DNA synthesis and inducing DNA single-strand breaks.
T18538 MAC glucuronide phenol-linked SN-38

Others Others
MAC glucuronide phenol-linked SN-38, a pH-sensitive lactone and DNA topoisomerase I inhibitor drug linker, exhibits cytotoxicity in L540cy and Ramos cells, with IC50 values of 113 ng/mL and 67 ng/mL, respectively[1].
T18722 MAC glucuronide α-hydroxy lactone-linked SN-38

Others Others
MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 drug linker. MAC glucuronide α-hydroxy lactone-linked SN-38 is cytotoxic across L540cy cells and Ramos cells
T73905 SN-38 glucuronide

SN-38 glucuronide为Irinotecan这一抗癌活性分子的非活性代谢物。Irinotecan是拓扑异构酶I抑制剂,主要应用于结肠癌及直肠癌的研究。
T38474 CL2-MMT-SN38

CL2-MMT-SN38

CL2-MMT-SN38 is a derivative of SN-38, which is a potent anticancer agent and the active metabolite of Irinotecan (CPT-11), a Topoisomerase I inhibitor.
T77882 SN38-COOH

SN38-COOH 是合成抗体-活性分子偶联物 (ADC) 的关键中间体。SN-38 作为伊立替康的活性代谢物,主要功能是抑制拓扑异构酶 I,从而阻碍 DNA 和 RNA 的合成。
T82710 CL2E-SN38

CL2E-SN-38为结构稳定的抗体与SN-38偶联物,属于抗体药物偶联物(ADC)。SN-38作为Irinotecan在喜树碱中的活性代谢产物,充当拓扑异构酶I抑制剂。
T77837 CL2E-SN38 TFA

CL2E-SN-38 TFA为一抗体-SN-38稳定偶联体,属抗体药物偶联物(ADC)范畴。SN-38是Irinotecan活性代谢产物,源自喜树碱,作为拓扑异构酶I的抑制剂。
T81143 SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3

SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3 是一款用于抗体药物偶联物 (ADC) 合成的化学试剂,由抗癌药物SN38与链接子Lys(MMT)-PAB-oxydiacetamide-PEG8-N3 构成,属于点击化学工具。该化合物含有Azide基团,它可通过铜催化的叠氮-炔点击反应 (CuAAc) 与含Alkyne基团的分子耦合,亦能通过应变促进的炔-叠氮点击反应 (SPAAC) 与含DBCO 或 BCN 基团的分子反应。
T4595 YHO-13177

YHO 13177,YHO13177

BCRP Membrane transporter/Ion channel
YHO-13177 是高活性乳腺癌耐药蛋白多药转运通道(BCRP)抑制剂,可增强SN-38活性。
T25593 Labetuzumab govitecan

IMMU-130,Labetuzumab-SN38,hMN14-SN38,IMMU130,IMMU 130

Others Others
Labetuzumab govitecan is an anti-CEACAM5/SN-38 antibody-drug conjugate for therapy of refractory or relapsing metastatic colorectal cancer.
T77824 Sacituzumab govitecan

IMMU-132

Sacituzumab govitecan (IMMU-132)是一种针对Trop-2的抗体-活性分子偶联物(ADC),其通过传递SN-38发挥抗癌活性。
T17730 CL2 Linker

Others Others
CL2 Linker is a cleavableADC linker. CL2-SN-38 and CL2A-SN-38 are equivalent in drug substitution (~6), cell binding (Kd ~1.2 nM), cytotoxicity (IC50 ~2.2 nM), and serum stability in vitro (t1/2 ~20 hours)[1][2].
T69193 SN-28049

SN-28049 SN is a DNA intercalating drug that binds selectively to GC-rich DNA and shows curative activity against the Colon 38 adenocarcinoma in mice. SN 28049 has a complex action that may involve poisoning of topo IIalpha, suppression of topo I and inhibition of gene transcription from promoters with SP-1 sites. These actions may contribute to the promising experimental solid tumour anticancer activity of SN 28049.
T27141 Delimotecan

MEN4901,MEN 4901,T-0128,MEN-4901,T 0128

Delimotecan is a DNA topoisomerase I inhibitor. Delimotecan had a long terminal half-life of 109 h, and relatively high exposures to T-2513 and SN-38 were obtained. The percentage decrease in WBC and absolute neutrophil count significantly correlated with
T37685 CAY10719

CAY10719

CAY10719 is a selective inhibitor of the breast cancer resistance protein ABCG2 (IC50 = 0.23 μM) with little activity at ABCG1. It has been shown to reverse the ABCG2-mediated resistance toward SN 38 and to inhibit ATPase activity.
T70577 PEN-866

PEN-866 is a potential agent for controlling early stage tumor growth for non-small cell lung cancer (NSCLC). PEN-866 is a novel esterase-cleavable conjugate of an HSP90i and a topoisomerase I inhibitor, SN-38
T38446 ROC-0929

ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s), effectively targeting hGX with an IC50 of 80 nM. It efficiently inhibits the phosphorylation of ERK1/2 and p-38. sPLA2s, belonging to the disulfide-rich, Ca2+-dependent enzyme family, catalyze the hydrolysis of glycero-phospholipids at the sn-2 position, resulting in the release of a fatty acid and a lysophospholipid. ROC-0929 holds promise in researching inflammation-related diseases.
T62097 UNC10201652

UNC10201652 是一种 L1 特异性肠道细菌 β-葡萄糖醛酸酶 (GUSs) 的有效抑制剂,能够作用于大肠杆菌 (E. coli) (IC50: 0.117 μM)。UNC10201652 只有在粪便肠道菌群 L1 GUS 酶高度丰富的个体中才可以阻断 SN-38 glucuronide 的加工。

化合物

CL2A-SN-38 DCA 1279680-68-0(free base)
Cat.No: T17731L
Synonym:
Target: Others
Mc-VC-PAB-SN38
Cat.No: T39222
Synonym: Mc-VC-PAB-SN38
Target: Others
CL2A-SN-38
Cat.No: T17731
Synonym:
Target: Others
CL2-SN-38
Cat.No: T10832
Synonym:
Target: Others
MC-SN38
Cat.No: T38962
Synonym: MC-SN38
Target:
MAC glucuronide phenol-linked SN-38
Cat.No: T18538
Synonym:
Target: Others
MAC glucuronide α-hydroxy lactone-linked SN-38
Cat.No: T18722
Synonym:
Target: Others
SN-38 glucuronide
Cat.No: T73905
Synonym:
Target:
CL2-MMT-SN38
Cat.No: T38474
Synonym: CL2-MMT-SN38
Target:
SN38-COOH
Cat.No: T77882
Synonym:
Target:
CL2E-SN38
Cat.No: T82710
Synonym:
Target:
CL2E-SN38 TFA
Cat.No: T77837
Synonym:
Target:
SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3
Cat.No: T81143
Synonym:
Target:
YHO-13177
Cat.No: T4595
Synonym: YHO 13177,YHO13177
Target: BCRP
Labetuzumab govitecan
Cat.No: T25593
Synonym: IMMU-130,Labetuzumab-SN38,hMN14-SN38,IMMU130,IMMU 130
Target: Others
Sacituzumab govitecan
Cat.No: T77824
Synonym: IMMU-132
Target:
CL2 Linker
Cat.No: T17730
Synonym:
Target: Others
SN-28049
Cat.No: T69193
Synonym:
Target:
Delimotecan
Cat.No: T27141
Synonym: MEN4901,MEN 4901,T-0128,MEN-4901,T 0128
Target:
CAY10719
Cat.No: T37685
Synonym: CAY10719
Target:
PEN-866
Cat.No: T70577
Synonym:
Target:
ROC-0929
Cat.No: T38446
Synonym:
Target:
UNC10201652
Cat.No: T62097
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T1703 SN-38

7-乙基-10-羟基喜树碱,NK012,伊立替康杂质B,SN 38

DNA/RNA Synthesis; Topoisomerase; Autophagy Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
SN-38 (NK012) 是 DNA 拓扑异构酶 I (Topo I) 抑制剂 Irinotecan 的活性代谢产物,可以抑制 DNA 和 RNA 合成 (IC50=0.077/1.3 μM)。SN-38 具有抗肿瘤活性,可以诱导细胞自噬。
T0486L Irinotecan Hydrochloride

盐酸伊立替康,伊立替康盐酸盐,Camptothecin 11 hydrochloride,CPT-11 hydrochloride

Topoisomerase; Autophagy Autophagy; DNA Damage/DNA Repair
Irinotecan Hydrochloride (CPT-11 hydrochloride) 是喜树碱半合成衍生物的盐酸盐,是一种拓扑异构酶 I 抑制剂,可研究结肠癌和直肠癌。
T6S1559 Aurantio-obtusin

Others Others
Aurantio-obtusin 是从决明子中分离出的蒽醌类化合物,具有抗炎、抗凝血、抗氧化、抗高血压的活性。它能抑制 IgE 介导的肥大细胞和过敏模型中的过敏反应,具有研究过敏相关疾病的潜力。在大鼠中,它通过内皮细胞 PI3K/AKT/ eNOS 依赖信号通路放松全身动脉,是潜在的新型血管扩张剂。
TQ0260 Cerulenin

Antibiotic; Antifungal; Fatty Acid Synthase Metabolism; Microbiology/Virology
Cerulenin 是广泛使用的天然脂肪酸合成酶抑制剂。它是由真菌Cephalosporium caeruleus 产生的。它抑制拓扑异构酶I 催化活性并增强 SN-38 诱导的细胞凋亡。它具有抗真菌和抗肿瘤活性。

天然产物

SN-38
Cat.No: T1703
Synonym: 7-乙基-10-羟基喜树碱,NK012,伊立替康杂质B,SN 38
Target: DNA/RNA Synthesis, Topoisomerase, Autophagy
Irinotecan Hydrochloride
Cat.No: T0486L
Synonym: 盐酸伊立替康,伊立替康盐酸盐,Camptothecin 11 hydrochloride,CPT-11 hydrochloride
Target: Topoisomerase, Autophagy
Aurantio-obtusin
Cat.No: T6S1559
Synonym:
Target: Others
Cerulenin
Cat.No: TQ0260
Synonym:
Target: Antibiotic, Antifungal, Fatty Acid Synthase
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