Cancer Targeted Therapy

Cancer targeted therapy is the foundation of precision medicine; it uses drugs or other substances to target specific genes and proteins that control cancer cells’ growth, division and spreading. Compared to traditional chemotherapy drugs, targeted-drugs can specifically act on cancer cells with high efficacy without damaging normal cells. Drugs used in cancer targeted therapy mainly includes small molecules and macromolecules (e.g., monoclonal antibodies), which can target cancer cells and constituents in the tumor microenvironment to activate the immune system. Anti-angiogenesis drugs, such as those targeting vascular endothelial growth factor (VEGF), epidermal growth factor receptor (EGFR), transforming growth factor (TGF)-α, TGF-β, Tumor necrosis factor (TNF)-α, and platelet-derived endothelial growth factor (PDGFR) inhibit the proliferation and metastasis of cancer cells. In recent years, the proportion of antibody drugs in cancer treatment has gradually become prominent. Antibody-drug conjugates (ADCs) are a new type of targeted drugs that are composed of monoclonal antibody, cytotoxic drug and linker. ADCs can deliver drugs to tumor cells and minimize the toxicity to normal tissues. Proteolysis-targeting chimera (PROTAC) is a useful technology for targeted protein degradation. PROTAC exploits the ubiquitin-proteasome system and forms a ternary complex with a hijacked E3 ubiquitin ligase and target protein, leading to polyubiquitination and degradation of the target protein.

Targeted therapy is a useful strategy in treatment of cancer either alone or in combination with standard chemotherapy. At present, targeted therapy has proved significant clinical success in the treatment of many types of cancer, including breast cancer, colorectal cancer, leukemia, ovarian cancer and lung cancer.

Cancer Targeted Therapy Related Products (35602):

Cat. No.	Product Name	CAS No.	Purity	Chemical Structure

HY-50910

Temsirolimus	162635-04-3	99.56%
Temsirolimus is an inhibitor of mTOR with an IC₅₀ of 1.76 μM. Temsirolimus activates autophagy and prevents deterioration of cardiac function in animal model.

HY-104042

Vorasidenib	1644545-52-7	99.87%
Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC₅₀ ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K. Vorasidenib can be used for the study of grade 2 astrocytoma or oligodendroglioma with a susceptible IDH1/2 mutation.

HY-B0649

Propofol	2078-54-8	99.52%
Propofol potently and directly activates GABA_A receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.

HY-15424

5-Iodotubercidin	24386-93-4	99.64%
5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC₅₀ of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin.

HY-18983

Calyculin A	101932-71-2	99.67%
Calyculin A ((-)-Calyculin A) is a potent and cell-permeable protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) inhibitor with IC₅₀s of 2 nM and 0.5-1 nM, respectively.

HY-10992

AZD-7762	860352-01-8	99.94%
AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC₅₀ of 5 nM for Chk1.

HY-14176

Compound E	209986-17-4	99.97%
Compound E is a γ-secretase inhibitor. Compound E blocks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC₅₀s of 0.24, 0.37, 0.32 nM, respectively.

HY-B1205

Atropine	51-55-8	99.85%
Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC₅₀ values of 0.39 and 0.71 nM for Human mAChR M₄ and Chicken mAChR M₄, respectively. Atropine inhibits ACh-induced relaxations in human pulmonary veins. Atropine can be used for research of anti-myopia and bradycardia.

HY-N1724

Concanamycin A	80890-47-7	≥99.0%
Concanamycin A (Folimycin; Antibiotic X 4357B) is a macrolide antibiotic, a vacuolar type H⁺-ATPase (V-ATPase) inhibitor. Concanamycin A is also an inhibitor of lysosomal acidification, can be used to T cell-mediated inflammation research^-.

HY-15036

Diclofenac	15307-86-5	99.92%
Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC₅₀s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.

HY-70013

Abiraterone	154229-19-3	99.88%
Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC₅₀s of 2.5 nM and 15 nM, respectively.

HY-13749

Sitagliptin	486460-32-6	99.75%
Sitagliptin (MK-0431) is a potent and orally active inhibitor of DPP4 with an IC₅₀ of 19 nM in Caco-2 cell extracts.

HY-134901

WM-3835	2229025-70-9	99.78%
WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice.

HY-P9915

Daratumumab	945721-28-8	99.10%
Daratumumab (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab has anti-multiple myeloma (MM) effect. Daratumumab impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition.

HY-Y0337

L-Cysteine	52-90-4
L-Cysteine (Cysteine) is an orally active conditionally essential amino acid with hypoglycemic effects, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine promotes the proliferation and differentiation of neural stem cells via the CBS/H2S pathway. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans. L-Cysteine can be used as an anorectic agent.

HY-19980

Eprenetapopt	5291-32-7	99.52%
Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.

HY-N0141

Parthenolide	20554-84-1	99.91%
Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.

HY-15001

Stemregenin 1	1227633-49-9	99.95%
Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC₅₀ of 127 nM.

HY-15826

SGC-CBP30	1613695-14-9	99.83%
SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (K_ds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects.

HY-15146

NSC 74859	501919-59-1	98.35%
NSC 74859 (S3I-201) is a selective Stat3 inhibitor with an IC₅₀ of 86 μM.

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