Cancer Targeted Therapy

Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC₅₀s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2.

1,4-Di(3-hydroxypropoxy)butane is the linker of PROTAC Aster-A degrader-1 (HY-D233) and can be used for the synthesis of PROTAC.

CRBN ligand-218 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-218 can be linked to a target protein ligand via a linker to form a PROTAC.

TH7299 is a TbFolD inhibitor with antiparasitic activity. TH7299 binds the tetrahydrofolate-binding pocket of MTHFD2, and inhibits MTHFD2L and the dehydrogenase/cyclohydrolase domain of MTHFD1. TH7299 reduces cancer cells viability, induces apoptosis, DNA damage. TH7299 can be used for the researches of african trypanosomiasis and acute myeloid leukemia.

BrAC-GGFG-Aminal-PI3K/mTOR-IN-21 is a conjugate of PI3K/mTOR-IN-21 (HY-185456) and Linker.

Nabumetone (Standard) is the analytical standard of Nabumetone (HY-B0559). This product is intended for research and analytical applications. Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the proagent of the active metaboliteα-Demethylnaproxen (HY-W086896). Nabumetone can inhibit cancer cells proliferation and relieve gastric ulcers.

Heptacosanedioic Acid is a PROTAC linker that can be used in the synthesis of PROTACs.

Benfluron hydrochloride is an Apoptosis inducer and inhibitor of the HIV-1 Rev-RRE complex, with an IC₅₀ of 5.0 μM against the HIV-1 Rev-RRE complex. Benfluron hydrochloride induces p53 activation, and triggers phosphorylation of Chk1 at serine 345, Chk2 at threonine 68, as well as ERK1/2 at threonine 202 and tyrosine 204. Benfluron hydrochloride activates Caspase 8, Caspase 9 and Caspase 3/7, inhibits HIV-1 viral transcription, and acts as a substrate for 11β-HSD 1 and cytosolic carbonyl reductase. Benfluron hydrochloride can be used in research related to leukemia and HIV-1 infection.

Chlorquinaldol (Standard) is the analytical standard of Chlorquinaldol. This product is intended for research and analytical applications. Chlorquinaldol (Chloquinan) is an antibacterial agent with the potential use in topical skin conditions and vaginal infections. Chlorquinaldol is a β-catenin/TCF4 inhibitor, showing anti-proliferation, anti-migration, and apoptosis-inducing activity in cancer cells.

GGTI-297 is a geranylgeranyl transferase I (GGTase-1) inhibitor with IC₅₀ values of 56 nM and 203 nM for GGTase-1 and fanesyl transferase (FTase), respectively. GGTI-297 inhibits the processing of the geranylgeranylated protein Rap1A without affecting the farnesylated protein H-Ras.

MMAF intermediate 1 is an intermediate in the synthesis of MMAF (HY-15579). MMAF (Monomethylauristatin F) is a potent inhibitor of tubulin polymerization and the cytotoxic (ADC Cytotoxin) component of classic antibody drug conjugates (ADCs), such as Vorsetuzumab mafodotin and SGN-CD19A.

CRBN ligand-739 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-739 can be linked to a target protein ligand via a linker to form a PROTAC.

Anhydro abiraterone is a degradation product of Abiraterone acetate (HY-75054). Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity.

Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC₅₀ values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC₅₀s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease. Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC₅₀ of 3.5 μM, can be used for the research of metabolic disorders.

Pinometostat (Standard) is the analytical standard of Pinometostat. This product is intended for research and analytical applications. Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.

Roblitinib (Standard) is the analytical standard of Roblitinib (HY-101568). This product is intended for research and analytical applications. Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity.

NSC 625987 (Standard) is the analytical standard of NSC 625987 (HY-103380). This product is intended for research and analytical applications. NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC₅₀ of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2.

CRBN ligand-408 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-408 can be linked to a target protein ligand via a linker to form a PROTAC.

CRBN ligand-241 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-241 can be linked to a target protein ligand via a linker to form a PROTAC.

KX2-361 (Standard) is the analytical standard of KX2-361 (HY-111187). This product is intended for research and analytical applications. KX2-361 (KX-02) is a Src-K_inase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell.