human lung cancer cell growth

Lumichrome 是人类体内的内源性化合物，由核黄素光降解产生。它利用p53 依赖机制抑制人肺癌细胞生长并诱导凋亡。

Triglycidyl isocyanurate (Teroxirone) 是一种三氮烯三环氧化合物，可通过 p53的激活抑制非小细胞肺癌细胞的生长。它诱导细胞凋亡，具有抗血管生成和抗肿瘤活性，用于癌症研究。

JBJ-08-178-01 作为一种选择性酪氨酸激酶抑制剂，特异性地针对人表皮生长因子受体2 (HER2) 的突变形态，表现出显著的抗肿瘤活性。该化合物通过促进肺癌中HER2受体的蛋白酶体降解，有效降低其激酶活性及蛋白表达量。在非小细胞肺癌治疗的研究中，JBJ-08-178-01 显示出了积极的治疗潜力。

SBI-183 是一种具有口服活性的 QSOX1 抑制剂 (Kd: 20 μM)，能够抑制肾癌细胞系、三阴性乳腺癌细胞系、肺腺癌细胞系和胰腺导管腺癌的增殖与侵袭表型。SBI-183 在体内可以抑制两种人肾细胞癌异种移植小鼠模型的肿瘤生长。

CEP-1612 is a proteasomal inhibitor responsible for the proteolysis of proteins that regulate important cell cycles and apoptosis. CEP-1612 can induce p21WAF1 and p27KIP1 expression and apoptosis, and inhibit tumor growth of human lung cancer.

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg ml) and Gram-negative bacteria (MICs = 136-200 µg ml), as well as yeasts (MICs = 10-20 µg ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16 BL6 mouse model of melanoma when administered at a dose of 25 mg kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg kg.3Ajoene (25 mg kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16 BL6 melanoma cells in C57BL 6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)

2-deoxy-D-Glucose-13C6is intended for use as an internal standard for the quantification of 2-deoxy-D-glucose by GC- or LC-MS. 2-deoxy-D-Glucose is a glucose antimetabolite and an inhibitor of glycolysis.1,2It inhibits hexokinase, the enzyme that converts glucose to glucose-6-phosphate, as well as phosphoglucose isomerase, the enzyme that converts glucose-6-phosphate to fructose-6-phosphate.32-deoxy-D-Glucose (16 mM) induces apoptosis in SK-BR-3 cells, as well as inhibits the growth of 143B osteosarcoma cells cultured under hypoxic conditions when used at a concentration of 2 mg ml.4,5In vivo, 2-deoxy-D-glucose (500 mg kg) reduces tumor growth in 143B osteosarcoma and MV522 non-small cell lung cancer mouse xenograft models when used alone or in combination with doxorubicin or paclitaxel .6 1.Kang, H.T., and Hwang, E.S.2-Deoxyglucose: An anticancer and antiviral therapeutic, but not any more a low glucose mimeticLife Sci.78(12)1392-1399(2006) 2.Aft, R.L., Zhang, F.W., and Gius, D.Evaluation of 2-deoxy-D-glucose as a chemotherapeutic agent: Mechanism of cell deathBr. J. Cancer87(7)805-812(2002) 3.Ralser, M., Wamelink, M.M., Struys, E.A., et al.A catabolic block does not sufficiently explain how 2-deoxy-D-glucose inhibits cell growthProc. Natl. Acad. Sci. USA105(46)17807-17811(2008) 4.Liu, H., Savaraj, N., Priebe, W., et al.Hypoxia increases tumor cell sensitivity to glycolytic inhibitors: A strategy for solid tumor therapy (Model C)Biochem. Pharmacol.64(12)1745-1751(2002) 5.Zhang, X.D., Deslandes, E., Villedieu, M., et al.Effect of 2-deoxy-D-glucose on various malignant cell lines in vitroAnticancer Res.26(5A)3561-3566(2006) 6.Maschek, G., Savaraj, N., Priebe, W., et al.2-deoxy-D-glucose increases the efficacy of adriamycin and paclitaxel in human osteosarcoma and non-small cell lung cancers in vivoCancer Res.64(1)31-34(2004)

Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1]. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer[1].Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process[2]. [1]. Moyer JD, et al. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. 1997, 57(21), 4838-4848.[2]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

Monoacylglycerols (MAGs) of ω-3 polyunsaturated fatty acids have diverse physiological and health effects. In particular, MAGs containing docosahexaenoic acid or eicosapentaenoic acid have anti-proliferative properties against colon and lung cancer cell lines. Eicosapentaenoyl 1-propanol-2-amide is an EPA-containing MAG amide analog that inhibits the growth of human lung carcinoma A549 cells, producing 98.4% growth inhibition when applied at 3 μM. It is an analog of eicosapentaenoyl ethanolamide , a natural N-acylethanolamide that impacts aging and inflammation.

Chromomycin A2 is an aureolic acid that has been found in several marine actinomycetes and has antibacterial and anticancer activities. Chromomycin A2 inhibits the growth of B. subtilis in an agar diffusion assay. It also inhibits the growth of human SGC7901 gastric cancer, HepG2 hepatocellular carcinoma, A549 lung epithelial adenocarcinoma, HCT116 colon cancer, and COC1 ovarian cancer cells, as well as human umbilical vein endothelial cells (HUVECs; IC50s = 4, 0.5, 3, 5, 5, and 8 nM, respectively). Chromomycin A2 (30 nM) halts the cell cycle in the G0/G1 phase and increases the protein levels of LC3A and LC3B in MALME-3M melanoma cells, indicating that it induces autophagy. It also increases the levels and promoter activity of the autophagic proteins ATG7 and ATG10 and reduces cell viability to 50% in human SCC-11 squamous cell carcinoma cells when used at a concentration of 30 nM.

KRC-108 is a multiple kinase inhibitor. KRC-108 is a potent inhibitor of Ron, Flt3 and TrkA as well as c-Met. KRC-108 inhibited oncogenic c-Met M1250T and Y1230D more strongly than wild type c-Met. The anti-proliferative activity of KRC-108 was measured by performing a cytotoxicity assay on a panel of cancer cell lines. The GI(50) values (i.e., 50% inhibition of cell growth) for KRC-108 ranged from 0.01 to 4.22 μM for these cancer cell lines. KRC-108 was also effective for the inhibition of tumor growth in human HT29 colorectal cancer and NCI-H441 lung cancer xenograft models in athymic BALB c nu nu mice. This molecule should serve as a useful lead for inhibitors targeting kinases and may lead to new therapeutics for the treatment of cancer. (source: Invest New Drugs. 2012 Apr;30(2):518-23. doi: 10.1007 s10637-010-9584-2. Epub 2010 Nov 16. ).

c-Myc inhibitor8 是一种 c-Myc 抑制剂。c-Myc inhibitor8 有效抑制多种癌细胞的细胞活力。c-Myc inhibitor8 在小鼠模型中抑制人前列腺癌和肺癌肿瘤的生长。c-Myc inhibitor8 可用于癌症研究。

Bavituximab (Anti-Human Phosphatidylserine Recombinant Antibody) 是一种针对磷脂酰丝氨酸 (PS) 的单克隆抗体，具有血管靶向和免疫调节特性，能够重新激活抗肿瘤免疫来抑制肿瘤生长。Bavituximab 具有抗癌活性，常联合Paclitaxel 和 Carboplatin 来研究非小细胞肺癌。

Necitumumab (IMC-11F8) 是一种针对表皮生长因子 （EGF） 受体的人单克隆抗体，是一种用于治疗晚期非小细胞肺癌的抗血管生成剂，可用于研究癌症。

MS934是一种VHL招募MEK1 2降解剂，能够有效抑制HT-29细胞生长，表现出抗增殖效果，其GI50值达到0.023 μM。该化合物适用于包括黑色素瘤、非小细胞肺癌(NSCLC)、结直肠癌、原发性脑肿瘤和肝细胞癌在内的多种人类癌症研究。

22-(4′-py)-JA是久那霉素A的半合成衍生物，源自泰国蓝海绵（Xestospongia sp.）。该化合物显示出抗转移活性，能抑制AKT mTOR p70S6K信号通路，并阻断人脐静脉内皮细胞（HUVEC）中肿瘤细胞侵袭及管形成作用。它通过下调金属蛋白酶（MMP-2和MMP-9）、缺氧诱导因子1α（HIF-1α）和血管内皮生长因子（VEGF）来发挥作用。此外，22-(4′-py)-JA对非小细胞肺癌（NSCLC）显示出显著的抗癌效果。

Mollicellin I（compound 1）为一种Depsidone类化合物。其对Bre04人乳腺癌细胞系、Lu04人肺癌细胞系以及N04人神经瘤细胞系的生长抑制活性低，GI50s均超过10 μg mL。

Mollicellin H, 次级代谢物源于真菌C. brasiliense，显示出免疫调节、细胞毒性和抗肿瘤等多种生物活性。它对三种人类癌细胞系——乳腺癌 (Bre04)、肺癌 (Lu04) 和神经瘤 (N04) 的生长抑制半数有效浓度 (GI50s) 分别为5.1 μg mL、6.5 μg mL 和2.5 μg mL。

(S)-Sabutoclax ((S)-BI-97C1) 作为一种光学纯的阿朴棉酚衍生物，对抗凋亡B细胞淋巴瘤 白血病2 (Bcl-2) 家族蛋白展现了全谱抑制作用。该化合物通过阻断BH3肽与Bcl-XL、Bcl-2、Mcl-1及Bfl-1的结合，展示出相应的IC50值为0.31、0.32、0.20及0.62 μM。此外，(S)-Sabutoclax还能有效抑制人类前列腺癌、肺癌以及淋巴瘤细胞系的生长，其EC50值分别为0.13、0.56及0.049 μM。因此，(S)-Sabutoclax对于基于细胞凋亡机制的癌症治疗研究具有重要价值。

1,4,5,6-Tetrahydroxy-7-prenylxanthone exhibits anti-cancer activity, demonstrating moderate cytotoxicity against breast cancer (MDA-MB-435S) and lung adenocarcinoma (A549) cell lines, with GI50 values of 2.

2β,3β,23α-Trihydroxy-12-oleanen-28-oic acid shows cytotoxic activities to human lung adenocarcinoma(A-549)cell lines. 2α,3β,23-Trihydroxyolean-12-en-28-oic acid and 2α,3β,23-trihydroxyurs-12-en-28-oic acid exhibit cytotoxicity in vitro against the growth of human cancer cells lines HepG-2,with IC50 values of 16.13 ± 3.83, 15.97 ± 2.47 uM, respectively.

Griffipavixanthone inhibits the growth of human Non-small-cell lung cancer H520 cells in dose- and time-dependent manners, it induces cell apoptosis through mitochondrial apoptotic pathway accompanying with ROS production. It can inhibit tumor metastasis

Dexylosyltubeimoside Ⅲ (compound 3) 是从 Actinostemma lobatum MAXIM 提取的环双糖苷，显示出对数种癌症细胞系具有抑制作用。在体外研究中，该化合物对人食管癌细胞系 ECA109 (IC50=22.37 μM)、肺癌细胞系 A549 (IC50=27.27 μM) 以及胃癌细胞系 MGC-803 (IC50=36.85 μM) 表现出抗癌活性。