Cancer Immunotherapy

PF-04217903 is an orally active, highly selective ATP-competitive c-Met kinase inhibitor with a K_i value of 4.8 nM and a K_d value of 4.5 nM. PF-04217903 blocks c-Met and HGF signaling pathways, inhibits MET phosphorylation, and blocks downstream MAPK, PI3K/AKT and PLCγ1 pathways. PF-04217903 suppresses tumor proliferation, survival, migration, invasion, angiogenesis and metastasis, induces apoptosis, and enhances efferocytosis, Annexin A1 expression and resolution of inflammation. PF-04217903 retains activity against several c-Met mutants (M1131T, V1220I, H1094R). PF-04217903 increases the incidence of subarachnoid hemorrhage and reduces survival rate without altering aneurysm formation, and also prevents lymph node metastasis induced by VEGF inhibition. PF-04217903 is applicable to research related to tumors (pancreas, stomach, lung, brain, colon, breast, kidney, melanoma, etc.), intracranial aneurysms and inflammatory diseases (gouty arthritis, neutrophilic pleuritis).

TBOPP is a selective inhibitor of DOCK1 with an IC₅₀ of 8.4 μM. TBOPP binds to the DOCK1 DHR-2 domain with high affinity (K_d of 7.1 μM), has anti-tumor activity for broader types of tumors.

inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties.

Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ET_A) receptor antagonist with a K_i of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research.

WK369 is a novel BCL6 small molecule inhibitor, which exhibits excellent anti-ovarian cancer bioactivity, induces cell cycle arrest and causes apoptosis. WK369 can directly bind to the BCL6-BTB domain and block the interaction between BCL6 and SMRT, leading to the reactivation of p53, ATR and CDKN1A.

Tropisetron is an orally active 5-HT3R antagonist (K_i = 5.3 nM) as well as being a potent and selective α7 nicotinic partial agonist (EC₅₀ = 1.3 μM). Tropisetron prevents phosphorylation and activation of the p38 MAPK. Tropisetron inhibits both IL-2 gene transcription and IL-2 synthesis in stimulated T cells. Tropisetron inhibits the binding to DNA and the transcriptional activity of NFAT and AP-1. Tropisetron is anti-inflammatory and antiemetic. Tropisetron has antitumor and neuroprotective effects. Tropisetron can be studied in research for diseases including hemorrhagic cystitis, chronic joint inflammation, lung cancer and chronic cerebral hypoperfusion.

CEP-40783 is a potent, selective and orally available inhibitor of AXL and c-Met with IC₅₀ values of 7 nM and 12 nM, respectively.

Lidocaine-d₁₀ is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia.

Varlilumab (CDX-1127) is an agonist anti-CD27 monoclonal antibody. Varlilumab can promote T cell expansion and activate the immune response. Varlilumab has anti-tumor activity and can be used in the research of hematological malignancies and solid tumors.

Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.

NSC139021 (ERGi-USU) is a RIOK2 inhibitor with anticancer activity. RIOK2 can highly selectively inhibit the growth of ERG-positive cancer cells with IC₅₀s of 30-400 nM against cell lines. RIOK2 also causes cell cycle arrest and apoptosis in glioblastoma via induction of Skp2 and Skp2-p27/p21-Cyclin E/CDK2-pRb signaling.

D-Glucuronic acid (Standard) is the analytical standard of D-Glucuronic acid. This product is intended for research and analytical applications. D-Glucuronic acid is a major component of many anti-inflammatory proteoglycans, which can promote embryonic development and inhibit cell aggregation. After being metabolized into ethyl glucuronide (HY-113093), D-Glucuronic acid activates Toll-like receptor 4 (TLR4), causing pain. D-Glucuronic acid and its derivative glucurono-lactone can serve as liver detoxifiers for human health prevention, and its derivatives also possess anti-tumor activity.

Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study.

Vevorisertib trihydrochloride (ARQ 751 trihydrochloride) is an orally active allosteric AKT inhibitor that blocks AKT phosphorylation. Vevorisertib trihydrochloride inhibits tumor cell proliferation through Cyclin D1 and Ki67. Vevorisertib trihydrochloride inhibits liver fibrosis through collagen accumulation, alpha-SMA, COL1, and TGF-beta. Vevorisertib trihydrochloride reduces total bilirubin. Vevorisertib trihydrochloride significantly reduces tumor size in a cirrhotic rat HCC model. Vevorisertib trihydrochloride can be used for research on hepatocellular carcinoma.

Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer.

Ascrinvacumab (PF-03446962) is a human IgG2 monoclonal antibody targets ALK-1. Ascrinvacumab shows binding efficiency with human ALK1 with a K_d value of 7 nM. Ascrinvacumab can be used for the research of hepatocellular carcinoma (HCC).

Nemvaleukin alfa (ALKS 4230) is a IL-2 fusion protein that selectively binds to intermediate-affinity IL-2R. Nemvaleukin alfa is an activator of NK and effector T cells. Nemvaleukin alfa can be used for research of cancer.

Olsalazine is an orally active prodrug of 5-ASA (HY-15027). Olsalazine can inhibit cells proliferation and induce apoptosis. Olsalazine can reduce DAI and MPO activity and inhibit inflammatory cytokines levels. Olsalazine can be used for the researches of cancer, inflammation and metabolic disease, such as colorectal cancer, inflammatory bowel disease (IBD) and hyperuricemic.

KA2507 is a potent, orally active and selective HDAC6 inhibitor, with an IC₅₀ of 2.5 nM. KA2507 shows antitumor activities and immune modulatory effects in preclinical models.

EG01377 is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a K_d of 1.32 μM, and IC₅₀s of both 609 nM for NRP1-a1 and NRP1-b1. EG01377 has antiangiogenic, antimigratory, and antitumor effects.