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 (35605):

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

HY-15414

Vortioxetine	508233-74-7	98.61%
Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial agonist of 5-HT_1B (K_i: 15 nM, 33 nM).

HY-138293

SY-5609	2417302-07-7	99.33%
SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a K_D of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (K_i=2600 nM), CDK9 (K_i=960 nM), CDK12 (K_i=870 nM). SY-5609 induces apoptosis in tumor cells and has antitumor activity.

HY-134964

CTB	451491-47-7	99.93%
CTB is a potent p300 histone acetyltransferase activator. CTB can effectively induce apoptosis in MCF-7 cells.

HY-N0292

Oleuropein	32619-42-4	99.05%
Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase.

HY-103096

R162	64302-87-0	99.98%
R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties.

HY-103259

Sodium metatungstate	12141-67-2
Sodium metatungstate (Sodium polyoxotungstate) is a NTPDase inhibitor, with K_i values of 2.58 μM, 3.26 μM, and 28.8 μM for NTPDase 1 (CD39), NTPDase 3 and NTPDase 2 respectively. Sodium metatungstate has anti-inflammatory and anti-cancer effect. Sodium metatungstate inhibits ATP breakdown but also blocks central synaptic transmission.

HY-108471

CU-CPT22	1416324-85-0	≥99.0%
CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam₃CSK₄) binding to TLR1/2 with a K_i of 0.41 µM. CU-CPT22 blocks Pam₃CSK₄-induced TLR1/2 activation with an IC₅₀ of 0.58 µM.

HY-132168

RMC-5552	2382768-62-7	99.94%
RMC-5552 is a potent and selective mTORC1 inhibitor. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC₅₀s of 0.14 nM and 0.48 nM, respectively. RMC-5552 shows much lower pAKT inhibition (IC₅₀ of 19 nM), resulting in mTORC1/mTORC2 selectivity approaching 40-fold. RMC-5552 has anti-cancer activity.

HY-13953

JIB-04	199596-05-9	98.29%
JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC₅₀s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.

HY-A0006

Pentostatin	53910-25-1	99.93%
Pentostatin (CI-825; Deoxycoformycin) is an irreversible inhibitor of adenosine deaminase with K_i of 2.5 pM.

HY-19609

Calicheamicin	108212-75-5	98.28%
Calicheamicin, an antitumor antibiotic, is a cytotoxic agent that causes double-strand DNA breaks. Calicheamicin is a DNA synthesis inhibitor. Calicheamicin is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-10572

Efavirenz	154598-52-4	99.93%
Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a K_i of 2.93 nM and exhibits an IC₉₅ of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture.

HY-13848

Rugocrixan	911715-90-7	99.54%
AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with K_is of 3.9 and 2800 nM, respectively.

HY-B0317

Amlodipine	88150-42-9	99.87%
Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer.

HY-B0022

Flutamide	13311-84-7	99.94%
Flutamide is an Androgen Receptor antagonist with Ki=55 nM. Flutamide inhibits prostate cancer progression and has synergistic effects with Docetaxel (HY-B0011). Flutamide also has the potential to protect against hyperthermia-induced multiple organ dysfunction syndrome.

HY-P3239

Belantamab mafodotin	2050232-20-5	99.78%
Belantamab mafodotin (GSK2857916) is composed of humanized and focused monoclonal antibody against B cell maturation antigen (BCMA) and McMMAF. The antibody portion is Belantamab (HY-P9980), and the drug-linker conjugate for ADC is McMMAF (HY-15578). Belantamab mafodotin has anti-myeloma activity.

HY-16931

SMIFH2	340316-62-3	99.08%
SMIFH2 is a formin specific inhibitor. SMIFH2 inhibits actin polymerization by Formins and affects the actin cytoskeleton.

HY-B0006

Carvedilol	72956-09-3	99.98%
Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC₅₀ of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.

HY-123942

Diprovocim	2170867-89-5	98.82%
Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC₅₀=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC₅₀=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses.

HY-107738

Guggulsterone	95975-55-6	99.83%
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC₅₀s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.

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