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Cat. No. | Product Name | Target | Signaling Pathways |
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T16369 |
O-Desmethyl gefitinib
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EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
O-Desmethyl gefitinib 是依赖于 CYP2D6 活性形成的,是 Gefitinib 在人血浆中的活性代谢产物。在亚细胞试验中,它抑制 EGFR,IC50为 36 nM。 | |||
T5437 |
Gefitinib-based PROTAC 3
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EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Gefitinib-based PROTAC 3 通过 linker 将 EGFR 结合元件与 von Hippel-Lindau 配体结合,在 HCC827(外显子 19 del)和 H3255(L858R 突变)细胞中诱导 EGFR 降解,DC50 分别为 11.7 和 22.3 nM。 | |||
T11384 |
Gefitinib-d8
ZD1839 D8,Gefitinib D8 |
Others | Others |
Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells. Gefitinib D8 is a deuterium labeled Gefitinib. | |||
T40785 |
Gefitinib impurity 1
|
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Gefitinib impurity 1 is a compound derived from Gefitinib, a potent and selective EGFR tyrosine kinase inhibitor (IC 50 = 33 nM). This orally active compound selectively inhibits tumor cell growth stimulated by EGF (IC 50 = 54 nM) and inhibits EGFR autophosphorylation induced by EGF in tumor cells. Additionally, Gefitinib induces autophagy and exhibits antitumor activity. | |||
T65550 |
Gefitinib analog III
4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl acetate |
Others | Others |
Gefitinib analog III (4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl acetate) 具有潜在的抗炎和抗肿瘤活性,可用于研究其在生物体内的相互作用和活性。 | |||
T1181L |
Gefitinib hydrochloride
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Gefitinib hydrochloride (ZD1839 hydrochloride) 是一种有效,选择性和具有口服活性的EGFR 酪氨酸激酶抑制剂,IC50为 33 nM。Gefitinib hydrochloride 选择性抑制 EGF 刺激的肿瘤细胞生长 (IC50为 54 nM),并阻断 EGF 刺激的肿瘤细胞中EGFR 自磷酸化。Gefitinib hydrochloride 也诱导细胞自噬 (autophagy),具有抗肿瘤活性。 | |||
T15268 |
FAAH-IN-2
O-Desmorpholinopropyl Gefitinib,4-(3-氯-4-氟苯氨基)-7-甲氧基喹唑啉-6-醇 |
FAAH; Autophagy | Autophagy; Metabolism; Neuroscience |
FAAH-IN-2 (O-Desmorpholinopropyl Gefitinib) 是一种脂肪酸酰胺水解酶的有效抑制剂。 | |||
T11385 |
Gefitinib N-oxide
|
Others | Others |
Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells. Gefitinib N-oxide is the N-oxide derivative of Gefitinib. | |||
T19489 | O-Desmethyl gefitinib D8 | EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
O-Desmethyl gefitinib D8 is a deuterium labeled O-Desmethyl gefitinib that is an active metabolite of Gefitinib in human plasma. | |||
T18316 |
MC-Sq-Cit-PAB-Gefitinib
|
Others | Others |
MC-Sq-Cit-PAB-Gefitinib is a potent antitumor drug-linker conjugate for Antibody-Drug Conjugates (ADC), utilizing Gefitinib—an EGFR tyrosine kinase inhibitor—connected through the MC-Sq-Cit-PAB ADC linker. | |||
T63630 |
Gefitinib dihydrochloride
|
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Gefitinib dihydrochloride 是有效的、选择性的、口服具有活力的 EGFR 酪氨酸激酶抑制剂 (IC50: 33 nM)。Gefitinib dihydrochloride 能够选择性抑制 EGF 刺激的肿瘤细胞生长,其IC50值为 54 nM,能够阻断 EGF 刺激的肿瘤细胞中EGFR 自磷酸化。Gefitinib dihydrochloride 可以诱导细胞自噬 (autophagy) 和凋亡 (apoptosis),能够用于进行癌症相关疾病,如肺癌和乳腺癌的研究。 | |||
T65585 |
Gefitinib impurity 5
|
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Gefitinib impurity 5 是一种有用的有机化合物,可用于生命科学领域的相关研究。其产品编号为 T65585,CAS号为 199327-61-2。 | |||
T73627 | Gefitinib N-oxide hydrochloride | ||
Gefitinib N-oxide hydrochloride 是 Gefitinib 的 N-oxide 衍生物。Gefitinib 是一种有效的 (EGFR) 抑制剂,在 NR6wtEGFR 细胞中 IC50值为 2-37 nM。 | |||
T67092 | Gefitinib impurity 2 | ||
Gefitinib impurity 2 是一种有用的有机化合物,可用于生命科学领域的相关研究,其产品编号为 T67092。 | |||
T81714 | N3-PEG8-Phe-Lys-PABC-Gefitinib | ||
N3-PEG8-Phe-Lys-PABC-Gefitinib是一种结合了抗癌活性分子Gefitinib(口服活性的抑制剂)与可降解的ADC linker N3-PEG8-Phe-Lys-PABC的点击化学试剂。该化合物具备Azide基团,能够通过铜催化的叠氮-炔环加成反应(CuAAc)与含Alkyne基团的分子反应,也可与含DBCO或BCN基团的分子进行菌株促进的炔-叠氮环加成反应(SPAAC)。 | |||
T77875 |
Mc-Val-Cit-PAB-Gefitinib chloride
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Mc-Val-Cit-PAB-Gefitinibchloride是一种担载EGFR酪氨酸激酶抑制剂Gefitinib的ADC活性分子连接子偶联物,由Gefitinib和专为ADC设计的连接子Mc-Val-Cit-PAB构成。 | |||
T6092 |
Sapitinib
沙普替尼,AZD-8931 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Sapitinib (AZD-8931) 是可逆的 ATP 竞争型 EGFR 抑制剂,对 EGFR、ErbB2 和 ErbB3的IC50值分别为4、3 和 4 nM。 | |||
T71436 |
D561-0775
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D561-0775 is a direct AMPK agonist, showing potential anti-cancer activity via inducing apoptosis, cell cycle arrest, suppressing glycolysis and cholesterol synthesis after activation of AMPK in gefitinib-resistant H1975 cells. | |||
T11157 |
EGFR-IN-1
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EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR-IN-1, an orally active and irreversible selective inhibitor targeting L858R/T790M mutant EGFR, exhibits strong antiproliferative and antitumor activity, particularly against H1975 cells and first line mutant HCC827 cells. This compound potently inhibits Gefitinib-resistant EGFR L858R/T790M mutations with a 100-fold selectivity over the wild-type EGFR. | |||
T75261 | EGFR-IN-1 TFA | ||
EGFR-IN-1 TFA 是一种口服活性不可逆的突变型选择性 L858R/T790MEGFR 抑制剂。与野生型 EGFR 相比,EGFR-IN-1 TFA 对 Gefitinib 耐药的 EGFRL858R/T790M 有 100 倍的抑制作用。EGFR-IN-1 TFA 对 H1975 细胞和 HCC827 细胞具有较强的抗增殖活性。具有抗肿瘤活性。 | |||
T78841 |
Nrf2-IN-3
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Nrf2-IN-3 (Compound R16) 为Nrf2抑制剂,与KEAP1突变体 (G333C mKEAP1) 结合,能够恢复受损的KEAP1/NRF2相互作用。该化合物通过修复mKEAP1/NRF2复合物,增加KEAP1突变癌细胞对Cisplatin和Gefitinib的敏感性。 | |||
T35147 |
WZ4002-hydroxy
WZ4002 analog, WZ4002 demethyl derivate,WZ 4002-hydroxy,WZ-4002-hydroxy |
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WZ4002-hydroxyl is a WZ4002 derivative or WZ4002 analogue in which methoxy is replaced by hydroxyl and can be detected in 50% of patients with clinical resistance to gefitinib or erlotinib. WZ4002 has a basic chemical skeleton (covalent pyrimidine) that d | |||
T41155 |
MS 154
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MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib(Iressa). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioa... | |||
T74457 | EGFR-IN-42 | ||
EGFR-IN-42 (Compound 17b) 是一种有效的 EGFR 抑制剂,具有单位数纳摩尔活性。EGFR-IN-42 通过共价键将他莫昔芬或安多昔芬与 EGFR 抑制剂吉非替尼连接起来。EGFR-IN-42 保留 ER 拮抗剂活性和 EGFR 抑制作用。EGFR-IN-42 具有优越的抗癌活性。 | |||
T74458 | EGFR-IN-43 | ||
EGFR-IN-43 (Compound 17c) 是一种有效的EGFR 抑制剂,具有单位数纳摩尔活性。EGFR-IN-43 通过共价键将他莫昔芬或安多昔芬与EGFR 抑制剂吉非替尼连接起来。EGFR-IN-43 保留 ER 拮抗剂活性和EGFR 抑制作用。EGFR-IN-43 具有优越的抗癌活性。 | |||
T69403 |
AZD-3409
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AZD-3409 is a potent prenyl transferase inhibitor. AZD-3409 showed higher potency than lonafarnib. The mean IC(50) for cytotoxicity of AZD3409 was 510 in MEF cells, 10,600 in A549 cells and 6,170 in MCF7 cells, respectively. In these cells, the IC(50) for FTase activity of AZD3409 ranged from 3.0 to 14.2 nM and of lonafarnib from 0.26 to 31.3 nM. AZD3409 inhibits farnesylation to a higher extent than geranylgeranylation. Both inhibition of farnesylation and geranylgeranylation could not be corre... | |||
T83890 |
Flavokawain 1i
Flavokavain 1i |
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Flavokawain 1i是chalcones的派生物,包括flavokawain A、flavokawain B和flavokawain C,具有抗癌和抗病毒活性。在30 µM浓度下,Flavokawain 1i能够抑制gefitinib抵抗性的H1975非小细胞肺癌(NSCLC)细胞的增殖率达到36%,同时降低热休克蛋白90(Hsp90)客体蛋白EGFR、c-Met、HER2、Akt和细胞周期依赖性激酶4(Cdk4)的蛋白水平,并提高Hsp70蛋白水平,这是Hsp90抑制的标志。肌肉内给药的Flavokawain 1i能够降低感染猪生殖与呼吸综合征病毒(PRRSV)猪只的病毒滴度。 | |||
T41156 |
MS 39
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MS 39是突变型表皮生长因子受体(EGFR)的高效、高亲和力和选择性降解剂,具有的高效、高亲和力和选择性。MS 39 由吉非替尼通过连接物偶联至 VHL 配体,能有效地诱导突变型 EGFR 的降解(在 HCC827(外显子19 del)和 H3255 (L858R 突变)肺癌细胞系中的 DC50值分别为5 nM 和3.3 nM),但在浓度高达10 μM 的野生型 EGFR 细胞系中无显著作用。MS 39在体外抑制 H3255肺癌细胞的增殖,并且在给药后在小鼠中具有生物利用性。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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T1181 |
Gefitinib
ZD1839,吉非替尼 |
EGFR; Tyrosine Kinases; Autophagy | Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Gefitinib (ZD1839) 是一种 EGFR 一代抑制剂,具有口服活性,抑制 EGFR 19 Del 和 L858R 突变。Gefitinib 具有抗肿瘤活性,用于治疗 EGFR 突变的非小细胞肺癌。Gefitinib 用药会产生 EGFR C797S 耐药突变。 |