Cat. No. | Product Name | Target | Signaling Pathways |
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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。 | |||
T76542 |
ErbB-2-binding peptide
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ErbB-2-binding peptide (HER2-binding peptide)为具结合肿瘤功能的肽类,其在癌症研究中显示出应用潜力。 | |||
T61272 | EGFR/HER2-IN-7 | ||
EGFR/HER2-IN-7 is a highly selective and potent anticancer compound specifically designed to target MCF-7 breast cancer cells. It functions as a dual inhibitor, targeting both EGFR/HER2 kinases and DHFR (dihydrofolate reductase). Its inhibitory activities are measured with IC50 values of 0.18 μM for EGFR, 0.146 μM for HER2, and 0.907 μM for DHFR [1]. | |||
T74468 |
MC-Val-Cit-PAB-Amide-TLR7 agonist 4
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MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) 是一种 HER2-TLR7和 HER2-TLR8免疫激动剂复合物。 | |||
T61596 | EGFR/HER2/DHFR-IN-1 | ||
EGFR/HER2/DHFR-IN-1 is a highly selective and potent anticancer compound specifically targeting MCF-7 breast cancer cells. It acts as a multi-inhibitor, targeting the EGFR/HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. Its mechanism of action involves cell cycle arrest at the G1/S phase and induction of apoptosis in cells [1]. | |||
T11938 |
Macropa-NH2 hydrochloride
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Others | Others |
Macropa-NCS, conjugated to Anti-Human HER2 and the prostate-specific membrane antigen-targeting compound RPS-070, serves as a promising therapeutic radionuclide for soft-tissue metastases treatment. Its precursor, Macropa-NH2 hydrochloride, facilitates its synthesis. | |||
T82492 | EGFR/HER2/DHFR-IN-3 | EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR/HER2/DHFR-IN-3(compound 4c)是一种针对EGFR和HER2的高效双重抑制剂,其IC50分别为0.138 μM和0.092 μM。该化合物同时对DHFR具有抑制作用,IC50为0.193 M。在生物活性方面,EGFR/HER2/DHFR-IN-3能够导致MCF7乳腺癌细胞周期在S期发生阻滞,并进而诱导细胞凋亡。 | |||
T72912 |
(R)-Afatinib
(R)-BIBW 2992 |
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(R)-Afatinib ((R)-BIBW 2992) 是 Afatinib 异构体。Afatinib 是一种口服有效且不可逆的 ErbB 家族 (EGFR 和HER2) 双特异性抑制剂,对 EGFRwt, EGFRL858R, EGFRL858R/T790M 和 HER2 的 IC50值分别为 0.5 nM、0.4 nM、10 nM 和 14 nM。Afatinib 可用于食管鳞状细胞癌 (ESCC)、非小细胞肺癌 (NSCLC) 和胃癌的研究。 | |||
T80955 |
Trastuzumab duocarmazine
(vic)-Trastuzumab duocarmazine |
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Trastuzumab duocarmazine ((vic)-Trastuzumab duocarmazine) 是一款HER2靶向ADC,它通过组织蛋白酶B的识别和裂解作用,选择性地作用于肿瘤细胞。此化合物在子宫和卵巢癌肉瘤等癌症的研究中显示出抗肿瘤活性。 | |||
T37329 |
PROTAC IDO1 Degrader-1
PROTAC IDO1 Degrader-1 |
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PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to CRBN E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells[1]. PROTAC IDO1 Degrader-1 (compound 2c) (10 μM; 24 hours) notably decreases IDO1 level induced by IFN-γ[1].PROTAC IDO1 Degrader-1 and IFN-γ (5 ng/mL) are incubated with HeLa cells for 24... |