pancreatic carcinoma

EIPA (L593754) 是一种 TRPP3 channel 抑制剂 (IC50=10.5 μM)，也是 Na+ H+交换 (NHE) 的抑制剂。EIPA 可以抑制巨胞饮作用，促进自噬，可用于炎症和肿瘤研究。

Daunorubicin hydrochloride (Rubidomycin hydrochloride) 是一种蒽环类氨基糖苷类化合物，一种拓扑异构酶 II (Topo II) 抑制剂。Daunorubicin hydrochloride 可以抑制 DNA 和 RNA 的合成，具有抗肿瘤活性。

Pyrazoloacridine (PD 115934) 是一种核酸结合剂，在 K562 细胞中抑制 topo I 和 II 的活性，IC50 为 1.25 μM。 Pyrazoloacridine 具有抗癌活性。

Berberine (Umbellatine) 属于生物碱类天然产物，可以激活 AMPK、抑制 DNA 拓扑异构酶、诱导 ROS 生成。Berberine 具有抗肿瘤、抗菌、降血糖、降血脂等生物学活性。

Broussochalcone A 是一种从桑科植物中提取的天然化合物，具有抗氧化和黄嘌呤氧化酶抑制活性（IC50 = 2.21 μM），能够清除自由基，抑制铁诱导的脂质过氧化，并减少脂多糖激活的巨噬细胞中一氧化氮的合成，也能够通过增加活性氧（ROS）水平和激活 FOXO3 信号通路，诱导人肾癌细胞凋亡。Broussochalcone A还是一种新型的 NR4A1 核受体抑制剂，能够通过 NR4A1 依赖的途径诱导胰腺癌细胞凋亡。

CU-T12-9 是特异性 TLR1 2激动剂，可激活先天免疫系统和适应性免疫系统。它选择性激活 TLR1 2 异二聚体，可通过促进 TLR1 和 TLR2 二聚而激活 NF-κB 信号，引起下游 TNF-α、IL-10 和 iNOS 增加。

UNBS3157是一种新型的非血液毒性萘酰亚胺衍生物，具有强大的抗肿瘤活性，能够通过DNA插入作用和毒化拓扑异构酶IIalpha来与DNA结合。与之相关的萘酰亚胺类化合物Amonafide在二期乳腺癌试验中表现出了活性，但由于限制剂量的骨髓毒性，目前尚未进入三期临床试验。相比之下，UNBS3157的最大耐受剂量比Amonafide高出3-4倍，并且在显示出显著抗肿瘤效果的剂量下未引起小鼠的血液毒性。此外，在活体内模型中，包括(i) L1210鼠白血病、(ii) MXT-HI鼠乳腺腺癌、以及(iii)人类A549非小细胞肺癌和BxPC3胰腺癌原位模型中，UNBS3157显示出优于Amonafide的效果。

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。

STAT3-IN-41 (Compound 16) 是 compound 1 的前药，能够缓慢释放抑制STAT3信号通路的 compound 1，并对肺癌、肝细胞癌和胰腺癌显示出抗肿瘤活性。

CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10736 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model.References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018). CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10736 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model. References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018).

CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16 F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16 F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10735 (5 mg kg) reduces tumor growth in B16 F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model.References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018). CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16 F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16 F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10735 (5 mg kg) reduces tumor growth in B16 F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model. References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018).

Potent EGFR-kinase inhibitor (IC50 = 0.7 nM). Displays >3000-fold selectivity against a panel of serine/threonine kinases. Reduces metastasis and angiogenesis in a mouse model of pancreatic cancer. Antihypertensive and orally bioavailable. Bruns et al (2000) Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 60 2926 PMID:10850439 |Ulu et al (2013) Epidermal growth factor receptor inhibitor PKI-166 governs cardiovascular protection without beneficial effects on the kidney in hypertensive 5/6 nephrectomized rats. J.Pharmacol.Exp.Ther. 345 393 PMID:23528611 |Kaspersen et al (2012) Activity of 6-aryl-pyrrolo[2,3-d]pyrimidine-4-amines to Tetrahymena. Bioorg.Chem. 44 35 PMID:22832269

Gastrin-releasing peptide (GRP) is a neuropeptide that stimulates gastrin release. It binds to (Ki = 300 nM) and stimulates amylase secretion in rat pancreatic AR42J cells (EC50 = 0.3 nM). GRP increases proliferation of human liver carcinoma HepG2 and MHCC97H cells but does not affect the proliferation of normal HL-7702 liver cells at a concentration of 1 nM. In vivo, GRP (0.35 nmol/kg/h) increases both pancreatic exocrine secretion and pancreatic polypeptide (PP) release in rats. It dose-dependently stimulates gastrin, pancreatic amylase, lipase, bilirubin, and acid output and induces gallbladder contraction in humans when administered at doses ranging from 1 to 27 pmol/kg per hour.

Toripalimab 是一个国产抗肿瘤 PD-1抗体。Toripalimab 是一种靶向 PD-1的选择性人源化单克隆抗体。Toripalimab 能够与 PD-1结合并阻断与其配体相互作用。Toripalimab 具有强效抗肿瘤作用，可用于黑色素瘤、肺癌、消化道肿瘤、肝胆和胰腺肿瘤、神经内分泌肿瘤、鼻咽癌和尿路上皮癌等肿瘤的研究。

WEE1-IN-8 (Compound 55) 作为一种高选择性的WEE1抑制剂,显示出优异的活性,其IC50仅为0.98 nM.此化合物适用于研究包括胰腺癌、卵巢癌、结肠癌及子宫浆液癌在内的多种癌症.

TBAP-001是RAF 激酶的泛抑制剂，IC50为 62 nM。

Vorsetuzumab mafodotin是一种人源化抗CD70单克隆抗体，结合了高效的合成药物负载物monomethyl auristatin F (MMAF)，运用了Seattle Genetics独有的抗体-药物偶联体(ADC)技术。CD70在多种实体肿瘤上有表达，包括肾细胞癌、胰腺癌、卵巢癌、肺癌、多发性骨髓瘤以及多种非霍奇金淋巴瘤。