advanced cancer

Aplidine possesses antiviral activity against SARS-CoV-2(IC90 = 0.88 nM). Aplidine is a potent anti-cancer agent by targeting eukaryotic translation elongation factor 1 Alpha 2(EEF1A2, Kd = 80 nM).

Sacituzumab govitecan (IMMU-132) is a humanized ADC compound targeting Trop-2 with anticancer activity for the study of refractory, locally advanced or metastatic breast cancer and uroepithelial cancer.

Valspodar (PSC 833) is a small-molecule inhibitor and a P-glycoprotein (P-gp) inhibitor with high selectivity and chemosensitizing properties. This compound can effectively reverse P-gp-mediated multidrug resistance (MDR) and is used in experimental research on drug-resistant tumors such as advanced epithelial ovarian cancer.

Avotaciclib (BEY1107) is a potent, orally active cyclin-dependent kinase 1 (CDK1) inhibitor, suitable for research in locally advanced or metastatic pancreatic cancer.

Camizestrant (Estrogen receptor antagonist 2) is an antagonist of the estrogen receptor and can be used in studies about ER+ HER2-advanced breast cancer[1].

Conteltinib (CT-707) is an enzyme inhibitor with antitumor activity targeting FAK, ALK, and Pyk2.Conteltinib exhibits significant inhibition of FAK, overcomes hypoxia-mediated sorafenib resistance in hepatocellular carcinoma through inhibition of YAP signaling, and can be used in advanced ALK-positive non-small-cell lung cancer and lymphoma.

Emitefur (BOF-A 2) is an orally active and potent 5-fluorouracil derivative with anticancer and antitumor activity.Emitefur is used in advanced gastric cancer, breast cancer and metabolism-related diseases.

Ataquimast is used in curing advanced receptor-positive breast cancer.

OB 24 hydrochloride is a selective, orally active HO-1 inhibitor (IC50=1.9 μM) exhibiting antitumor and anti-metastatic properties, suitable for studying prostate cancer, melanoma, ovarian cancer, and lung cancer metastasis.

Enloplatin is a carboplatin analog that has a partial role in advanced ovarian cancer.

Lapatinib (GW572016) is an inhibitor of ErbB2 and EGFR (IC50=9.2/10.8 nM) with oral activity. Lapatinib has antitumor activity and can be used to treat advanced or metastatic breast cancer with HER2 overexpression.

Lapatinib ditosylate (Lapatinib tosilate) monohydrate is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib ditosylate monohydrate therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury.

Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

AZD0022 is a selective, reversible, and orally active KRAS G12D inhibitor exhibiting high affinity for both active (KRAS G12D-GTP) and inactive (KRAS G12D-GDP) proteins, whilst demonstrating selectivity for wild-type KRAS. AZD0022 exhibits tumour marker inhibition in PDAC and NSCLC models, making it suitable for investigating tumours such as advanced solid tumours, pancreatic cancer, and colorectal cancer.

Durvalumab (MEDI 4736) is a humanized monoclonal antibody targeting PD-L1. It can block the interaction of PD-L1 with PD-1 and CD80, with IC50 values of 0.1 and 0.04 nM, respectively. Durvalumab is often used in combination with platinum-based compounds for the treatment of non-small cell lung cancer and advanced hepatocellular carcinoma cells.

Glufosfamide is a novel oxazolophosphamide compound with anticancer activity for the study of advanced non-small cell lung cancer.

NSC745885 is an antitumor agent non-toxic to normal cells that downregulates EZH2 via proteasome-mediated degradation. It exhibits toxicity against multiple normal and drug-resistant cancer cell lines and may be used in studies of advanced bladder cancer and oral squamous cell carcinoma.

Treosulfan (NSC 39069) is a bifunctional alkylating agent used in the treatment of advanced ovarian cancer.[2]

VZ185 is a potent, fast-acting, and selective von Hippel–Lindau–based dual degrader probe targeting BRD9 and BRD7 with DC50 values of 4.5 nM and 1.8 nM, respectively. VZ185 displays marked cytotoxicity in EOL-1 and A-402 cell lines with EC50 values of 3 nM and 40 nM, enabling advanced studies of chromatin remodeling, targeted protein degradation, and cancer cell dependency on SWI/SNF complex components.

LY2090314, an effective GSK-3α/β inhibitor (IC50: 1.5 nM/0.9 nM), may improve the efficacy of platinum-based chemotherapy regimens. LY2090314 has been used in trials studying the treatment of Leukemia, Advanced Cancer, and Pancreatic Cancer.

KRASG12C IN-13 (LY3499446), a potent inhibitor of KRAS G12C, shows potential in the study of advanced solid tumors, specifically non-small cell lung cancer and colorectal cancer.

GSK2636771, an effective, specific, orally bioavailable, PI3Kβ inhibitor, has been used in cancer, lymphoma, solid neoplasm, recurrent solid neoplasm, and advanced malignant neoplasm.

EGFR-IN-91 (compound 9) is an orally active EGFR inhibitor capable of crossing the blood-brain barrier. It effectively inhibits EGFRL858R/C797S and EGFRexon 19del/C797S, leading to tumor regression in patient-derived xenograft (PDX) mouse models. EGFR-IN-91 shows potential for inhibiting locally advanced and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutations.

SJL2-1 is a PRMT5 inhibitor with an IC50 value of 1.56 μM. It suppresses the proliferation, migration, and invasion of prostate cancer cells and induces apoptosis while causing cell cycle arrest at the G0/G1 phase. SJL2-1 targets intracellular PRMT5, inhibiting androgen receptor methylation and expression. It is applicable in research on early androgen-sensitive prostate cancer and advanced castration-resistant prostate cancer (CRPC).