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17

抑制剂 & 化合物

6

天然产物

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Cat. No. Product Name Target Signaling Pathways
T70959 Irinotecan Carboxylate Sodium Salt

Irinotecan Carboxylate Sodium Salt is a DNA topoisomerase inhibitor.
T70957 NMac1

NMac1is a small molecule phenylbutenoid dimer that has novel anti-proliferative effect only under glucose starvation in metastatic breast cancer cells. NMac1 causes significant activation of AMPK by decreasing ATP synthesis, lowers mitochondrial membrane potential (MMP, ΔΨm), and inhibits oxygen consumption rate (OCR) under glucose starvation. These effects of NMac1 are provoked by a consequence of OXPHOS complex I inhibition.
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.
T31837 FOLFIRI Regimen

FOLFIRI

FOLFIRI Regimen is a chemotherapy regimen consisting of leucovorin calcium (calcium folinate), 5-fluorouracil, and irinotecan used during the treatment of advanced-stage and metastatic colorectal cancer.
T81924 LK-44

hCES2A-IN-2 (Compound 44) 为口服活性人羧酸酯酶 2 (hCES2A) 抑制剂,IC50 值为5.02 μM,能够有效改善Irinotecan 引起的迟发性腹泻。
T70312 AZ1366

AZ1366 is a potent tankyrase inhibitor that enhances irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance. Combination AZ1366 and irinotecan achieved greater anti-tumor effects compared to monotherapy. Activity was limited to CRC explants that displayed irinotecan resistance and increased protein levels of tankyrase and NuMA.
T12766 RPR121056

APC

AChR Neuroscience
RPR121056 is a Irinotecan metabolite, which is generated by CYP3A4. Irinotecan is an antineoplastic agent that inhibits topoisomerase type I.
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。
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.
T74491 Antitumor agent-61

Antitumor agent-61 (Compound 9b),Irinotecan (Ir)的衍生物,展现出对多种肿瘤细胞(包括SK-OV-3、SK-OV-3/CDDP、U2OS、MCF-7、A549与MG-63)具有显著的抑制效果,其IC50值分别为0.92、1.39、1.75、2.20、3.05和3.23 μM。该化合物主要通过线粒体途径引发SK-OV-3细胞的凋亡。
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。
T82231 hCES2-IN-1

hCES2-IN-1(Compound 24)是一种选择性的hCES2可逆抑制剂,其IC50值为6.72 μM。该化合物能够减少活细胞中hCES2的表达量,并且能有效抵抗由Irinotecan引起的迟发性腹泻以及DSS诱发的溃疡性结肠炎。
T35942 AZ 5704

Potent and selective ATM kinase inhibitor (IC50 = 0.6 nM in an enzyme inhibition assay). Exhibits > 600-fold selectivity for ATM over other kinases. Inhibits ATM kinase in an in vitro cellular assay (IC50 = 0.33 μM). Potentiates the antitumor effects of the topoisomerase 1 inhibitor irinotecan in tumor bearing, immunocompromised mice. Orally bioavailable. Degorce et al (2016) Discovery of novel 3-quinoline carboxamides as potent, selective and orally bioavailable inhibitors of ataxia telangiecta...
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。
T95359 Compound F0433-0067

hiCE inhibitor-1是一种磺胺衍生物,是一种选择性的人体肠道酶 (hiCE) 抑制剂,Ki 值为 53.3 nM。hiCE inhibitor-1可用于改善 Irinotecan 引起的腹泻。
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。
T79263 Antitumor agent-102

Topoisomerase DNA Damage/DNA Repair
Antitumor agent-102(compound 10)是拓扑异构酶 I(topoisomerase I)抑制剂SN38与葡萄糖转运蛋白(glucose transporter)抑制剂缀合物,专门针对结直肠癌。相较于伊立替康,该化合物在肿瘤组织中可诱导游离SN38的更高浓度。

化合物

Irinotecan Carboxylate Sodium Salt
Cat.No: T70959
Synonym:
Target:
NMac1
Cat.No: T70957
Synonym:
Target:
CL2-MMT-SN38
Cat.No: T38474
Synonym: CL2-MMT-SN38
Target:
FOLFIRI Regimen
Cat.No: T31837
Synonym: FOLFIRI
Target:
LK-44
Cat.No: T81924
Synonym:
Target:
AZ1366
Cat.No: T70312
Synonym:
Target:
RPR121056
Cat.No: T12766
Synonym: APC
Target: AChR
CL2E-SN38 TFA
Cat.No: T77837
Synonym:
Target:
MC-SN38
Cat.No: T38962
Synonym: MC-SN38
Target:
Antitumor agent-61
Cat.No: T74491
Synonym:
Target:
SN-38 glucuronide
Cat.No: T73905
Synonym:
Target:
hCES2-IN-1
Cat.No: T82231
Synonym:
Target:
AZ 5704
Cat.No: T35942
Synonym:
Target:
CL2E-SN38
Cat.No: T82710
Synonym:
Target:
Compound F0433-0067
Cat.No: T95359
Synonym:
Target:
SN38-COOH
Cat.No: T77882
Synonym:
Target:
Antitumor agent-102
Cat.No: T79263
Synonym:
Target: Topoisomerase
Cat. No. Product Name Target Signaling Pathways
T6228 Irinotecan

CPT-11,Topotecin,伊立替康,(+)-Irinotecan

Topoisomerase; Autophagy Autophagy; DNA Damage/DNA Repair
Irinotecan (CPT-11) 是喜树碱的衍生物,是一种 DNA 拓扑异构酶 I (Topo I) 的抑制剂。Irinotecan 通过与 Topo I 复合物结合来阻止 DNA 链的重新连接,并导致双链 DNA 断裂和细胞死亡,具有抗肿瘤活性。
T0486 Irinotecan hydrochloride trihydrate

Irinotecan HCl Trihydrate,CPT-11 HCl Trihydrate,盐酸伊立替康三水合物

Topoisomerase; Autophagy Autophagy; DNA Damage/DNA Repair
Irinotecan hydrochloride trihydrate (CPT-11 HCl Trihydrate) 通过抑制拓扑异构酶 1 来防止 DNA 展开,可研究结肠癌和直肠癌。
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。
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。
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。
TN1783 Isolicoflavonol

异甘草黄酮醇

Lipid Metabolism
Isolicoflavonol 以可逆和混合的方式抑制人羧酸酯酶2介导的荧光素二乙酸酯水解, Ki 小于1.0 μM。

天然产物

Irinotecan
Cat.No: T6228
Synonym: CPT-11,Topotecin,伊立替康,(+)-Irinotecan
Target: Topoisomerase, Autophagy
Irinotecan hydrochloride trihydrate
Cat.No: T0486
Synonym: Irinotecan HCl Trihydrate,CPT-11 HCl Trihydrate,盐酸伊立替康三水合物
Target: 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
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
Aurantio-obtusin
Cat.No: T6S1559
Synonym:
Target: Others
Isolicoflavonol
Cat.No: TN1783
Synonym: 异甘草黄酮醇
Target: Lipid
TargetMol Loading
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