Cancer Targeted Therapy

Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC₅₀s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrochloride hydrate exhibits antitumor efficacy.

RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction.

NCT-506 is an orally bioavailable aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with an IC₅₀ of 7 nM.

Quetmolimab (E6011) is a humanized anti-Fractalkine (CX3CL1) monoclonal antibody. Quetmolimab binds to membrane-bound and soluble Fractalkine, neutralizes Fractalkine-induced migration of CX3CR1-expressing cells, mediates target-bound complex elimination from serum. Quetmolimab suppresses free soluble Fractalkine levels in cynomolgus monkeys, with target engagement linked to increased serum total Fractalkine concentration. Quetmolimab can be used for the research of Crohn’s disease, rheumatoid arthritis, and primary biliary cholangitis.

Pomalidomide-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology. Pomalidomide-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

CC-90002 is a humanized anti-CD47 monoclonal antibody (mAb). CC-90002 has a high affinity for binding to CD47 with a subnanomolar K_d value. CC-90002 can be used for the research of hematologic malignancies and solid tumors.

EPZ004777 hydrochloride is an effective and selective DOT1L inhibitor, with IC₅₀ being 0.4 nM. EPZ004777 hydrochloride reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 hydrochloride selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 hydrochloride can be used for the study of leukemia.

Vixtimotamab (AMV-564; TandAb T564) is a bispecific tetravalent tandem diabody (TandAb) that targets human CD33 and human CD3 antigens. Vixtimotamab can be used for the research of acute myeloid leukemia (AML).

FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC₅₀ of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions.

Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (K_i=31 nM, IC₅₀=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma.

Yadanziolide A, isolated from the cultivated dry seeds of Brucea javanica, has strong antiviral activities with IC₅₀ of 5.5 μM against tobacco mosaic virus. Yadanziolide A shows significant antitumor effects.

3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases.

Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.

FANCM-BTR PPI-IN-1 (Compound 32) is a FANCM/BTR interaction inhibitor that blocks the localization of FANCM to telomeres. FANCM-BTR PPI-IN-1 exhibits anticancer activity against osteosarcoma.

HDAC9-IN-1 is a selective class IIa HDAC inhibitor that binds to HDAC9 with an IC₅₀ of 40 nM. HDAC9-IN-1 potently inhibits HDACs 4 and 7 while showing weak activity against HDAC6 (IC₅₀ values: 180 nM (HDAC4), 190 nM (HDAC7), 970 nM (HDAC6)). HDAC9-IN-1 significantly inhibits several human cancer cells, induces apoptosis and DNA damage in human cancer cells, and modulates caspase-related proteins and p38 in human cancer cells. HDAC9-IN-1 can be used for the research of oral cancer, breast cancer, gastric cancer.

Doxycycline hydrochloride (Standard) is the analytical standard of Doxycycline hydrochloride (HY-N0565A). This product is intended for research and analytical applications. Doxycycline hydrochloride is an orally active highly lipophilic, tissue-permeable MMP inhibitor with broad-spectrum antibacterial activity. Doxycycline hydrochloride is also a semi-synthetic antibiotic with chelating properties, which blocks bacterial protein synthesis and inhibits extracellular matrix degradation through interactions with zinc and calcium atoms. Doxycycline hydrochloride also inhibits mitochondrial biogenesis, translation, and the expression of respiratory chain proteins. Doxycycline hydrochloride induces apoptosis, inhibits autophagy and EMT, downregulates stem cell markers, and activates the PI3K-AKT pathway, thereby effectively inhibiting the viability and proliferation of cancer cells such as breast cancer cells. Doxycycline hydrochloride also promotes the survival and self-renewal of embryonic stem cells and neural stem cells, and reduces the frequency of medium changes in culture. Doxycycline hydrochloride has been applied in studies related to breast cancer, prostate cancer, bladder cancer, and other cancers.

NGM-120 is a fully humanized IgG1 monoclonal antibody targeting GFRAL, which functions by blocking the GDF15-GFRAL axis. NGM-120 reduces serum GDF15 levels, increases body weight, expands central memory and proliferative CD8⁺ T cell populations, and decreases immunosuppressive and naive regulatory T cell populations. NGM-120 can be used for research on advanced prostate cancer.

ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206) , highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K⁺ channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation. Ex/Em=587/615 nm.
Solvent and concentration: DMSO: 1 mM

Bersanlimab (BI-505) is a fully human monoclonal antibody that targets intercellular adhesion molecule-1 (ICAM-1 or CD54). Bersanlimab has anticancer effects.

Br-PEG3-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.