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Search Results for " adc payload "

37

抑制剂 & 化合物

9

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T14348	Auristatin E	Microtubule Associated	Cytoskeletal Signaling
	Auristatin E 通过阻断微管蛋白的聚合来抑制细胞分裂。它是一种细胞毒性微管蛋白修饰剂，具有强效和选择性抗肿瘤活性。它是一种 MMAE 类似物，是抗体-药物偶联物中的细胞毒素。
T38889	Thailanstatin A
	Thailanstatin A 是真核 RNA 剪接抑制剂，IC50为650 nM，通过非共价结合到剪接体的 U2 snRNA 亚复合物的 SF3b 亚单位发挥作用。Thailanstatin A 对多种癌细胞系的抑制显示 nM 级别的 IC50。它与 Trastuzumab 上的赖氨酸结合，可产生“无连接子” ADC。
T11249L	Dxd Exatecan derivative for ADC,OQM5SD32BQ,UNII-OQM5SD32BQ	Topoisomerase	DNA Damage/DNA Repair
	Dxd (OQM5SD32BQ) 是一种有效的DNA 拓扑异构酶 I 抑制剂，IC50值为 0.31 μM，用作HER2靶向ADC 的偶联药物。
T14349	Auristatin F	Microtubule Associated	Cytoskeletal Signaling
	Auristatin F 是一种有效的微管抑制剂和血管损伤剂。 Auristatin F 可用于抗体-药物偶联物。
T15141	DM4 Ravtansine,美登素 DM4	Others; Microtubule Associated	Cytoskeletal Signaling; Others
	DM4 (Ravtansine)可用于制备抗体药物偶联物，是抗微管蛋白剂。它抑制细胞分裂。
T11120	Duocarmycin TM	DNA Alkylation; Antibiotic	DNA Damage/DNA Repair; Microbiology/Virology
	Duocarmycin TM 是一种有抗肿瘤活性的抗生素，也是一种 DNA 烷化剂。
T3256	MMAF 一甲基澳瑞他汀 F,MonoMethyl auristatin F	Others; Microtubule Associated	Cytoskeletal Signaling; Others
	MMAF (MonoMethyl auristatin F) 是一种抗有丝分裂剂，通过阻断微管蛋白的聚合来抑制细胞分裂，用作抗肿瘤药物和抗体偶联药物的细胞毒性成分。
T12081	MMAF-OMe Monomethyl auristatin F methyl ester
	MMAF-OMe (Monomethyl auristatin F methyl ester) 是一种抗微管蛋白剂，能够抑制 MDAMB435/5T4，MDAMB361DYT2，MDAMB468 和 Raji (5T4-) 这四种肿瘤细胞，IC50值分别为 0.056 nM，0.166 nM，0.183 nM 和 0.449 nM。它也是ADC 细胞毒素。
T8003	Methotrexate disodium	Apoptosis; Dehydrogenase; DNA/RNA Synthesis; Antifolate	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
	Methotrexate disodium 是一种叶酸类似物代谢抑制剂，具有免疫抑制剂和抗肿瘤特性，用于类风湿关节炎和研究多种癌症。
T16557	PNU-159682	Topoisomerase	DNA Damage/DNA Repair
	PNU-159682 是蒽环类新霉素的代谢产物，是一种 DNA 拓扑异构酶 II 抑制剂，具有出色的细胞毒性。
T1992	Mertansine DM1,Maytansinoid DM1	Microtubule Associated	Cytoskeletal Signaling
	Mertansine (DM1) 是一种微管蛋白抑制剂，也是一种抗体可缀合的美登木素生物碱。它通过连接体连接到单克隆抗体上，形成抗体偶联药物。
T14858	Calicheamicin Calicheamicin γ1,卡奇霉素	Others	Others
	Calicheamicin (Calicheamicin γ1) 是肿瘤抗生素，可引起DNA 双链断裂，抑制DNA 合成。
T21408	DM1-SMe DM1-SSMe	Microtubule Associated	Cytoskeletal Signaling
	DM1-SMe (DM1-SSMe) 是美登木素微管的有效抑制剂。 DM1-SMe 的效力是母体药物美登素的 3 至 10 倍，在一组人类肿瘤细胞系中，DM1-SMe 的 IC50 为 0.003 至 0.01 nM。
T6897	Monomethyl auristatin E 一甲基澳瑞他汀E,Vedotin,MMAE	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	Monomethyl auristatin E (MMAE) 是海兔毒素 10 的合成衍生物，是一种抗有丝分裂剂，通过阻断微管蛋白的聚合来抑制细胞分裂，并且还具有抑制抗体-药物偶联物的活性。
T1910	Ansamitocin P 3' Maytansinol butyrate,Ansamitocin P-3,安丝菌素P-3,Antibiotic C 15003P3'	Microtubule Associated	Cytoskeletal Signaling
	Ansamitocin P 3' (Maytansinol butyrate) 是一种具有抗肿瘤活性的抗体-药物偶联细胞毒素。
T4677	MMAD Monomethylauristatin D,Demethyldolastatin 10,单甲基澳瑞他汀 D,Monomethyl Dolastatin 10	Microtubule Associated	Cytoskeletal Signaling
	MMAD (Demethyldolastatin 10) 是一种有效的微管蛋白抑制剂，是抗体药物偶联物中的一种毒素有效载荷。
T11917	Lys-SMCC-DM1 Lys-Nε-MCC-DM1	Microtubule Associated	Cytoskeletal Signaling
	DM1 是一种微管蛋白抑制剂。 Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) 是 DM1 的活性代谢物。
T1485	Methotrexate NCI-C04671,WR19039,Amethopterin,甲氨蝶呤,CL14377	Apoptosis; Dehydrogenase; DNA/RNA Synthesis; Antifolate	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
	Methotrexate (WR19039) 是一种叶酸类似物，一种二氢叶酸还原酶 DHFR 的抑制剂。Methotrexate 具有抗代谢、抗肿瘤和免疫抑制等活性，常用于类风湿关节炎和多种肿瘤的研究。
T12149	N-Me-L-Ala-maytansinol	Others	Others
	N-Me-L-Ala-maytansinol used for making antibody-drug conjugate (ADC),is a hydrophobic, cell permeable payload.
T40049	MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin
	MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin (compound 21a), is a camptothecin payload which can be utilized in the synthesis of a camptothecin antibody-drug conjugate (ADC) by conjugation to a monoclonal antibody (mAb).
T81144	SMP-93566
	SMP-93566为一抗体-药物偶联物（Antibody-Drug Conjugates (ADCs)），其有效载荷（payload）脱落率低，可在体内抑制卵巢癌、胃癌及乳腺癌肿瘤。
T18701	SPDB-DM4	Others	Others
	SPDB-DM4 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) applications, employing the maytansine-based payload DM4 (a tubulin inhibitor) connected through a SPDB linker. This compound demonstrates significant anti-tumor efficacy.
T81146	SMP-33693
	SMP-33693为一种抗体-药物偶联物（Antibody-Drug Conjugates (ADCs)），其有效载荷（payload）稳定性高，显示出对卵巢癌、胃癌及乳腺癌肿瘤的体内抑制作用。
T15872	m-PEG4-Br	Others	Others
	m-PEG4-Br is a cleavable ADC linker used in the synthesis of antibody-drug conjugate (ADC) for Trastuzumab. m-PEG4-Br is placed distally from the monomethyl auristatin E (MMAE) payload to yield an ADC with altered hydrophilicity, antigen binding, and in v
T39458	DGN549-C DGN549-C
	DGN549-C is a novel compound featuring a cleavable ADC (antibody-drug conjugate) linker composed of valine-alanine (va) and a PBD (pyrrolobenzodiazepine) dimer. This compound possesses a unique DNA-alkylating cytotoxic payload, DGN549, which is utilized in the development of ADCs.
T18477	NAMPT inhibitor-linker 1	Others	Others
	NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.
T79206	MC-EVCit-PAB-MMAE
	MC-EVCit-PAB-MMAE (Linker-Payload 11) 作为一种ADC (drug-linker conjugates) 的代表，由具有功能性的ADC linker (MC-EVCit-PAB) 以及作为有效药物负载的微管蛋白聚合抑制剂MMAE组成。
T77910	Patritumab deruxtecan U3-1287,HER3-DXd
	Patritumab deruxtecan (HER3-DXd)为一抗体-药物偶联物（ADC），其结构为全人源IgG1单克隆抗体Patritumab通过含四肽的裂解性连接子与拓扑异构酶 I 抑制剂药效团相连。
T74940	Anticancer agent 81	Apoptosis	Apoptosis
	Anticanceragent 81（Compound 37b3）是用于诱导肿瘤细胞发生周期阻滞和凋亡（apoptosis）的化合物。当Anticanceragent 81作为有效载荷与Trastuzumab结合时，可生成抗体药物偶联物（ADC）T-PBA，此ADC保留了Trastuzumab的靶向特性和内化功能。
T78638	Clezutoclax
	Clezutoclax为Bcl-XL抑制剂且作为活性载体，可应用于抗体药物偶联物（ADC）的合成。
T18478	NAMPT inhibitor-linker 2	Others	Others
	NAMPT inhibitor-linker 2, a drug-linker conjugate for antibody-drug conjugates (ADCs), comprises an NAMPT inhibitor payload and a linker. When combined with an anti-c-Kit monoclonal antibody to form ADC-4, it demonstrates potent efficacy against c-Kit expressing cell lines, including GIST-T1 and NCI-H526, with IC50 values of <7 pM and 40 pM, respectively.
T75086	Dazostinag
	Dazostinag (TAK-676 free base) 为干扰素基因刺激剂 (STING) 蛋白的激动剂，展现出抗肿瘤活性。它能作为有效载荷 (payload) 用于合成抗体偶联活性分子 (ADC) 的构建。
T74562	Nampt-IN-10 trihydrochloride
	Nampt-IN-10 trihydrochloride (compound 4) 为磷酸核糖转移酶 (NAMPT) 抑制剂。在A2780与CORL23细胞中展现出活性，IC50值依次为5和19 nM。Nampt-IN-10 trihydrochloride 同时作为抗体偶联活性分子 (ADC) 的非限制性有效载荷。
T18522	PC Mal-NHS carbonate ester	Others	Others
	PC Mal-NHS carbonate ester is a cleavable linker specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1]. This chemical compound plays a crucial role in facilitating the conjugation of drugs to antibodies, enabling targeted delivery and enhanced efficacy of therapeutic agents. Its unique carbonate ester structure allows for efficient cleavage in the targeted environment, ensuring the controlled release of the drug payload. Its application in ADC synthesis highlights its imp...
T75134	MC-GGFG-AM-(10Me-11F-Camptothecin)
	MC-GGFG-AM-(10Me-11F-Camptothecin) 是ZW251合成的Linker-Payload偶联物。ZW251是靶向人GPC3的抗体-活性分子偶联物(ADC)，包括人源化IgG1抗体、喜树碱(camptothecin)类的扑异构酶1抑制剂ZD06519及连接子（马来酰亚胺锚定和甘酰甘酰苯丙酰甘氨酸(GGFG)-氨基甲基(AM)可切割连接体）。该药物对人和食蟹猴GPC3具高亲和力，在表达GPC3的HCC细胞系中快速内化并可对GPC3阴性癌细胞进行旁观者介导杀伤。
T38503	(2-pyridyldithio)-PEG1-hydrazine (2-pyridyldithio)-PEG1-hydrazine
	(2-Pyridyldithio)-PEG1-hydrazine is a one-unit cleavable polyethylene glycol (PEG) linker specifically designed for the synthesis of antibody-drug conjugates (ADCs). This linker offers the advantage of controlled release of the drug payload from the ADC construct. It is utilized in the conjugation process between the antibody and the cytotoxic drug, enabling the targeted delivery of the drug to cancer cells. The (2-pyridyldithio) group of this linker provides stability during circulation in the ...
T82021	Izeltabart IMGC-936
	Izeltabart（IMGC-936）是一款针对ADAM9的基于Maytansinoid的ADC，由与DM21-C位点特异性偶联的高亲和力人源化抗体构成，使Maytansinoid微管破坏载体通过稳定的三肽连接子进行传递，达到药物-抗体比约为2.0。Izeltabart在ADAM9阳性人类肿瘤细胞系上显示出明显的细胞毒性，并在动物异种移植肿瘤模型中展现出显著的抗肿瘤效果。

化合物

Cat.No: T14348

Target: Microtubule Associated

Thailanstatin A

Cat.No: T38889

Cat.No: T11249L

Synonym: Exatecan derivative for ADC,OQM5SD32BQ,UNII-OQM5SD32BQ

Target: Topoisomerase

Cat.No: T14349

Target: Microtubule Associated

Cat.No: T15141

Synonym: Ravtansine,美登素 DM4

Target: Others, Microtubule Associated

Cat.No: T11120

Target: DNA Alkylation, Antibiotic

Cat.No: T3256

Synonym: 一甲基澳瑞他汀 F,MonoMethyl auristatin F

Target: Others, Microtubule Associated

Cat.No: T12081

Synonym: Monomethyl auristatin F methyl ester

Methotrexate disodium

Cat.No: T8003

Target: Apoptosis, Dehydrogenase, DNA/RNA Synthesis, Antifolate

Cat.No: T16557

Target: Topoisomerase

Cat.No: T1992

Synonym: DM1,Maytansinoid DM1

Target: Microtubule Associated

Cat.No: T14858

Synonym: Calicheamicin γ1,卡奇霉素

Target: Others

Cat.No: T21408

Synonym: DM1-SSMe

Target: Microtubule Associated

Monomethyl auristatin E

Cat.No: T6897

Synonym: 一甲基澳瑞他汀E,Vedotin,MMAE

Target: Apoptosis, Microtubule Associated

Ansamitocin P 3'

Cat.No: T1910

Synonym: Maytansinol butyrate,Ansamitocin P-3,安丝菌素P-3,Antibiotic C 15003P3'

Target: Microtubule Associated

Cat.No: T4677

Synonym: Monomethylauristatin D,Demethyldolastatin 10,单甲基澳瑞他汀 D,Monomethyl Dolastatin 10

Target: Microtubule Associated

Cat.No: T11917

Synonym: Lys-Nε-MCC-DM1

Target: Microtubule Associated

Cat.No: T1485

Synonym: NCI-C04671,WR19039,Amethopterin,甲氨蝶呤,CL14377

Target: Apoptosis, Dehydrogenase, DNA/RNA Synthesis, Antifolate

N-Me-L-Ala-maytansinol

Cat.No: T12149

Target: Others

MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin

Cat.No: T40049

Synonym: MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin

Cat.No: T81144

Cat.No: T18701

Target: Others

Cat.No: T81146

Cat.No: T15872

Target: Others

Cat.No: T39458

Synonym: DGN549-C

NAMPT inhibitor-linker 1

Cat.No: T18477

Target: Others

MC-EVCit-PAB-MMAE

Cat.No: T79206

Patritumab deruxtecan

Cat.No: T77910

Synonym: U3-1287,HER3-DXd

Anticancer agent 81

Cat.No: T74940

Target: Apoptosis

Cat.No: T78638

NAMPT inhibitor-linker 2

Cat.No: T18478

Target: Others

Cat.No: T75086

Nampt-IN-10 trihydrochloride

Cat.No: T74562

PC Mal-NHS carbonate ester

Cat.No: T18522

Target: Others

MC-GGFG-AM-(10Me-11F-Camptothecin)

Cat.No: T75134

(2-pyridyldithio)-PEG1-hydrazine

Cat.No: T38503

Synonym: (2-pyridyldithio)-PEG1-hydrazine

Cat.No: T82021

Synonym: IMGC-936

Cat. No.	Product Name	Target	Signaling Pathways
T0968	Paclitaxel Taxol,紫杉醇,NSC 125973	Apoptosis; Microtubule Associated; Autophagy	Apoptosis; Autophagy; Cytoskeletal Signaling
	Paclitaxel (Taxol) 属于天然产物，是一种微管聚合物稳定剂。Paclitaxel 具有抗肿瘤活性；通过诱导有丝分裂停滞、细胞凋亡、细胞自噬等，导致细胞死亡。
T16016	Maytansinol 美登醇,Ansamitocin P-0	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	Maytansinol (Ansamitocin P-0) 在体外抑制微管组装并导致微管分解。它与辐射联用，用于果蝇和人类癌细胞。
TP1180	Dolastatin 10 尾海兔素10,NSC 376128,DLS 10	Microtubule Associated	Cytoskeletal Signaling
	Dolastatin 10 (DLS 10) 是一种多肽，可以抑制微管蛋白聚合，显示除抗有丝分裂的活性。
T1123	Camptothecin NSC-100880,Campathecin,喜树碱,(S)-(+)-Camptothecin,CPT	Apoptosis; Influenza Virus; Topoisomerase; Antibiotic; Antifungal	Apoptosis; DNA Damage/DNA Repair; Microbiology/Virology
	Camptothecin (CPT) 属于生物碱类天然产物，是一种 DNA 拓扑异构酶 I (Topo I) 的抑制剂 (IC50=679 nM)，具有特异性。Camptothecin 具有抗肿瘤活性，可以诱导细胞凋亡。
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。
T1020	Doxorubicin hydrochloride Adriamycin,Doxorubicin (Adriamycin) HCl,Hydroxydaunorubicin hydrochloride,盐酸多柔比星,盐酸阿霉素,NSC 123127	Apoptosis; Mitophagy; HBV; HIV Protease; Topoisomerase; Antibacterial; Antibiotic; AMPK; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Doxorubicin hydrochloride (Adriamycin) 属于蒽环类抗生素，是人类 DNA 拓扑异构酶 I/II 抑制剂 (IC50=0.8/2.67 μM)。Doxorubicin hydrochloride 具有细胞毒性和抗肿瘤活性。Doxorubicin hydrochloride 可降低 AMPK 及其下游靶蛋白乙酰辅酶 A 羧化酶的磷酸化，还可诱导凋亡和自噬。
T1511	Daunorubicin hydrochloride Daunomycin HCl,盐酸佐柔比星,盐酸柔红霉素,RP-13057 Hydrochloride,Rubidomycin hydrochloride,Daunorubicin HCl,Daunomycin	Apoptosis; DNA/RNA Synthesis; Topoisomerase; Antibacterial; Antibiotic; Autophagy	Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology
	Daunorubicin hydrochloride (Rubidomycin hydrochloride) 是一种蒽环类氨基糖苷类抗肿瘤药物，可抑制 DNA 复制和修复以及 RNA 和蛋白质合成。
T5749	10-Deacetyl-7-xylosyl paclitaxel 10-Deacetyl-7-xylosyltaxol,10-Deacetyltaxol 7-Xyloside,7-Xylosyl-10-deacetyltaxol,7-木糖甙-10-脱乙酰基紫杉醇,10-Deacetylpaclitaxel 7-Xyloside	Others; Microtubule Associated	Cytoskeletal Signaling; Others
	10-Deacetyl-7-xylosyl paclitaxel (7-Xylosyl-10-deacetyltaxol) 是一种紫杉醇衍生物，具有改进的药理特性和更高的水溶性，用于治疗癌症。
T1456	Doxorubicin Hydroxydaunorubicin,阿霉素,Adriamycin	Topoisomerase; AMPK	Chromatin/Epigenetic; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	Doxorubicin (Adriamycin) 是一种有细胞毒性的蒽环类抗生素，具有肿瘤化疗作用。它抑制DNA 拓扑异构酶 I 和拓扑异构酶 II，IC50分别为0.8 μM 和2.67 μM，从而抑制 DNA 复制。它下调AMPK 的基础磷酸化以及下游 acetyl-CoA 羧化酶。它诱导凋亡和自噬。

天然产物

Cat.No: T0968

Synonym: Taxol,紫杉醇,NSC 125973

Target: Apoptosis, Microtubule Associated, Autophagy

Cat.No: T16016

Synonym: 美登醇,Ansamitocin P-0

Target: Apoptosis, Microtubule Associated

Cat.No: TP1180

Synonym: 尾海兔素10,NSC 376128,DLS 10

Target: Microtubule Associated

Cat.No: T1123

Synonym: NSC-100880,Campathecin,喜树碱,(S)-(+)-Camptothecin,CPT

Target: Apoptosis, Influenza Virus, Topoisomerase, Antibiotic, Antifungal

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

Doxorubicin hydrochloride

Cat.No: T1020

Synonym: Adriamycin,Doxorubicin (Adriamycin) HCl,Hydroxydaunorubicin hydrochloride,盐酸多柔比星,盐酸阿霉素,NSC 123127

Target: Apoptosis, Mitophagy, HBV, HIV Protease, Topoisomerase, Antibacterial, Antibiotic, AMPK, Autophagy

Daunorubicin hydrochloride

Cat.No: T1511

Synonym: Daunomycin HCl,盐酸佐柔比星,盐酸柔红霉素,RP-13057 Hydrochloride,Rubidomycin hydrochloride,Daunorubicin HCl,Daunomycin

Target: Apoptosis, DNA/RNA Synthesis, Topoisomerase, Antibacterial, Antibiotic, Autophagy

10-Deacetyl-7-xylosyl paclitaxel

Cat.No: T5749

Synonym: 10-Deacetyl-7-xylosyltaxol,10-Deacetyltaxol 7-Xyloside,7-Xylosyl-10-deacetyltaxol,7-木糖甙-10-脱乙酰基紫杉醇,10-Deacetylpaclitaxel 7-Xyloside

Target: Others, Microtubule Associated

Cat.No: T1456

Synonym: Hydroxydaunorubicin,阿霉素,Adriamycin

Target: Topoisomerase, AMPK

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