Search Result

Results for "

orthotopic

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adenylate Cyclase (1) Akt (1) Apoptosis (8) Autophagy (1) c-Met/HGFR (1) Carbonic Anhydrase (4) CDK (1) COX (2) DNA/RNA Synthesis (1) EGFR (2) Endogenous Metabolite (1) Epigenetic Reader Domain (1) ERK (1) FAK (1) Ferroptosis (2) HDAC (4) Histone Methyltransferase (1) Interleukin Related (2) MDM-2/p53 (1) MHC (1) Microtubule/Tubulin (2) Mps1 (1) PROTACs (1) Protein Arginine Deiminase (1) Ras (1) Reactive Oxygen Species (ROS) (1) Reference Standards (1) Ser/Thr Kinase (1) TREM receptor (1) Wnt (2)
By Research Areas:	Cancer (32) Cardiovascular Disease (1) Inflammation/Immunology (3)

By Targets:

Adenylate Cyclase (1)

Akt (1)

Apoptosis (8)

Autophagy (1)

c-Met/HGFR (1)

Carbonic Anhydrase (4)

CDK (1)

COX (2)

DNA/RNA Synthesis (1)

EGFR (2)

Endogenous Metabolite (1)

Epigenetic Reader Domain (1)

ERK (1)

FAK (1)

Ferroptosis (2)

HDAC (4)

Histone Methyltransferase (1)

Interleukin Related (2)

MDM-2/p53 (1)

MHC (1)

Microtubule/Tubulin (2)

Mps1 (1)

PROTACs (1)

Protein Arginine Deiminase (1)

Ras (1)

Reactive Oxygen Species (ROS) (1)

Reference Standards (1)

Ser/Thr Kinase (1)

TREM receptor (1)

Wnt (2)

By Research Areas:

Cancer (32)

Cardiovascular Disease (1)

Inflammation/Immunology (3)

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-110243

CAIX Inhibitor S4 1 Publications Verification	Carbonic Anhydrase	Cancer
CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a K_i of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (K_i=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth .

HY-168555

YJ1206	CDK PROTACs Apoptosis	Cancer
YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC₅₀ of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker) .

HY-19350

BML-210 2 Publications Verification	HDAC Apoptosis	Cancer
BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC₅₀ of ∼5 µM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 induces apoptosis and displays antitumour activities in orthotopic mammary tumours in mice .

HY-115677

ILK-IN-3	Ser/Thr Kinase	Cancer
ILK-IN-3 is an orally active integrin linked kinase (ILK) inhibitor. ILK-IN-3 improves the anticancer efficacy of Docetaxel (HY-B0011) in orthotopic LCC6 model .

HY-12401A

Mps1-IN-3 hydrochloride 1 Publications Verification	Mps1	Cancer
Mps1-IN-3 hydrochloride is a potent and selective Mps1 inhibitor with an IC₅₀ value of 50 nM. Mps1-IN-3 hydrochloride can inhibit the proliferation of glioblastoma cells, and effectively sensitizes glioblastomas to Vincristine in orthotopic glioblastoma xenograft model .

HY-114483

AES-135 1 Publications Verification	HDAC	Cancer
AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC₅₀s ranging from 190-1100 nM .

HY-149035

PAA4	Others	Cancer
PAA4 is a methide carbon-centered polynuclear Au(I) clusters. PAA4 shows antiproliferative activity. PAA4 increases the expression of pH2AX in a time dependent manner. PAA4 shows anti-tumor effect in orthotopic bladder cancer mouse model .

HY-16444

Sagopilone ZK-EPO; ZK 219477	Microtubule/Tubulin	Cancer
Sagopilone (ZK-EPO) demonstrated antitumor activity in human orthotopic glioma models both in vitro and in vivo .

HY-P991621

EOS006215 EOS-215	TREM receptor	Cancer
EOS006215 is a humanized monoclonal antibody inhibitor targeting TREM-2. EOS006215 reprograms TREM2 ⁺ macrophages, significantly blocks their pleiotropic pro-tumoral functions and overcomes resistance. EOS215 decreases metastasis burden in orthotopic 4T1 triple negative breast cancer mice model and significantly inhibits tumor growth in anti-PD-1 resistant mice model. EOS006215 can be used to study advanced malignant solid neoplasm, such as triple negative breast cancer (TNBC) .

HY-P11058

OVA(250-264) OVAp	MHC	Cancer
OVA(250-264) (OVAvac) (OVAp) is an antigen peptide that can be from ovalbumin (OVA) presented by the class I MHC molecule, H-2Kb. OVA(250-264) combined withαMSLN (anti-MSLN antibody) significantly induces antigen-specific CD8 ⁺ T cell generation and infiltration for enhancing antitumor efficacy in orthotopic pancreatic cancer mice model. OVA(250-264) can be used for neoantigen vaccine development in pancreatic cancer immunotherapy research .

HY-155249

KGP591	Microtubule/Tubulin	Cancer
KGP591 is a tubulin polymerization inhibitor (IC₅₀ 0.57 µM). KGP591 induces significant G2/M stagnation, inhibits cell migration, disrupts microtubule structure and cell morphology in MDA-MB-231 cells. KGP591 shows antitumor activity in orthotopic model of kidney cancer (RENCA) .

HY-103193

NKH477 Colforsin dapropate hydrochloride	Adenylate Cyclase	Cardiovascular Disease
NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts .

HY-143411

GEM144	HDAC Apoptosis DNA/RNA Synthesis	Cancer
GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts .

HY-16726

Polmacoxib CG100649	COX Carbonic Anhydrase	Cancer
Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC₅₀ around 0.1 μg/ml) and carbonic anhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .

HY-16726R

Polmacoxib (Standard) CG100649 (Standard)	Reference Standards COX Carbonic Anhydrase	Cancer
Polmacoxib (Standard) is the analytical standard of Polmacoxib. This product is intended for research and analytical applications. Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC₅₀ around 0.1 μg/ml) and carbonic anhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .

HY-P99908

Efineptakin alfa NT-17	Interleukin Related	Cancer
Efineptakin alfa (NT-17) is a long-acting recombinant human IL-7. Efineptakin alfa supports the proliferation and survival CD4 ⁺ and CD8 ⁺ cells in both human and mice. Efineptakin alfa can be used for glioblastoma research .

HY-122844B

Ifebemtinib tosylate BI-853520 tosylate; IN-10018 tosylate	FAK	Cancer
Ifebemtinib (tosylate) (BI-853520 (tosylate); IN-10018 (tosylate)) is a highly selective PTK2 kinase inhibitor. Ifebemtinib (tosylate) demonstrates anti-tumor activity. Ifebemtinib (tosylate) inhibits FAK autophosphorylation in prostate carcinoma cells. Ifebemtinib (tosylate) can inhibit spheroid formation and orthotopic tumor growth in vivo. Ifebemtinib (tosylate) can be studied in anticancer research such as solid tumors, breast cancer, and malignant pleural mesothelioma .

HY-13545B

ABT-510 acetate	Apoptosis	Inflammation/Immunology Cancer
ABT-510 acetate is an anti-angiogenic TSP peptide (Thrombospondin-1 analogue) that induces apoptosis and inhibits ovarian tumour growth in an orthotopic, syngeneic model of epithelial ovarian cancer. ABT-510 acetate also reduces angiogenesis and inflammatory responses in a murine model of inflammatory bowel disease. ABT-510 acetate can be used in studies of cancer (particularly epithelial ovarian cancer) and inflammatory bowel disease (IBD) .

HY-13545

ABT-510	Apoptosis	Inflammation/Immunology Cancer
ABT-510 is an anti-angiogenic TSP peptide (Thrombospondin-1 analogue) that induces apoptosis and inhibits ovarian tumour growth in an orthotopic, syngeneic model of epithelial ovarian cancer. ABT-510 also reduces angiogenesis and inflammatory responses in a murine model of inflammatory bowel disease. ABT-510 can be used in studies of cancer (particularly epithelial ovarian cancer) and inflammatory bowel disease (IBD) .

HY-16785

Veledimex INXN-1001; RG-115932	Interleukin Related	Inflammation/Immunology Cancer
Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys .

HY-149036

PAA5	Ferroptosis Endogenous Metabolite Reactive Oxygen Species (ROS)	Cancer
PAA5 is a methide carbon-centered polynuclear Au(I) cluster. PAA5 can release Au(I) causing Pro-oxidant response and accelerated ferroptosis. PAA5 increases the expression of pH2AX in a time-dependent manner. PAA5 has anticancer activity .

HY-173433

JV8	Epigenetic Reader Domain	Cancer
JV8 is a BRD4 PROTAC degrader. JV8 promotes the ubiquitination and degradation of BRD4 and induces apoptosis. JV8 has antitumor activity in a mouse 4T1 orthotopic tumor model. (Pink: BRD4 ligand (HY-78695); Blue: E3 ligase VHL ligand (HY-173435); Black: Linker (HY-33366); E3 ligase VHL ligand-linker conjugate (HY-173436)) .

HY-P1416

Foxy-5 Maximum Cited Publications 6 Publications Verification	Wnt	Cancer
Foxy-5, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .

HY-161954

HDAC8-IN-12	HDAC	Cancer
HDAC8-IN-12 (compound 5k) is a non-hydroxamic acid, selective inhibitor of HDAC8 (IC₅₀: 0.12 nM) and a potent inhibitor of breast cancer. HDAC8-IN-12 triggers anti-tumor immunity by activating T cells, increasing the proportion of M1 macrophages and decreasing the proportion of M2 macrophages. HDAC8-IN-12 (50 mg/kg) exerts tumor suppressive effects in an orthotopic mouse model of breast cancer .

HY-P1416A

Foxy-5 TFA Maximum Cited Publications 6 Publications Verification	Wnt	Cancer
Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .

HY-170321

Apoptosis inducer 31	Apoptosis	Cancer
Apoptosis inducer 31 (compound 19) induces caspase-dependent apoptosis. Apoptosis inducer 31 plays an important role in cancer research .

HY-P991660

ARGX-111	c-Met/HGFR	Cancer
ARGX-111 is an afucosylated anti-MET antibody. ARGX-111 blocks HGF-dependent and -independent signaling, downregulating MET expression on the tumor cell surface. ARGX-111 depletes MET-expressing circulating tumor cells through enhanced antibody-dependent cell-mediated cytotoxicity (ADCC), thereby inhibiting tumor metastasis. ARGX-111 depletes circulating tumor cells and inhibits bone and lung metastasis in an orthotopic mouse model of metastatic breast cancer. ARGX-111 is promising for research in breast cancer and other cancers .

HY-173116

DOTA-XYIMSR-01	Carbonic Anhydrase	Cancer
DOTA-XYIMSR-01 is a molecular probe targeting CAIX that can be labeled with 177Lu for the inhibition and localization of malignant gliomas. The uptake of [177Lu] Lu-XYIMSR-01 in U87MG tumors is 6.19 % of the injected dose per gram (% ID/g), and the tumor-to-muscle uptake ratio is 20.14. In the orthotopic glioma model, combined injection with Temozolomide (HY-17364) can significantly improve the survival rate of mice and inhibit tumor growth. DOTA-XYIMSR-01 shows promise for research in the field of anti-cancer therapy .

HY-162494

PAD4-IN-4	Protein Arginine Deiminase	Cancer
PAD4-IN-4 (compound 28) is a potent PAD4 inhibitor (IC₅₀=0.79±0.09 μM). PAD4-IN-4 improves the tumor immune microenvironment by reshaping neutrophil phenotype, upregulating the proportions of dendritic cells and M1 macrophages, and reducing the amount of myeloid-derived suppressor cells. PAD4-IN-4 can be used for Triple-negative breast cancer research .

HY-148409

MMRi62	Ferroptosis Apoptosis Autophagy MDM-2/p53	Cancer
MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .

HY-163434

PRMT5/EGFR-IN-1	EGFR Histone Methyltransferase	Cancer
PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC₅₀s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .

HY-116504

WB-308	EGFR Akt ERK Apoptosis	Cancer
WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.

HY-12875

BQU57	Ras	Cancer
BQU57 is a selective inhibitor of RalA/RalB small GTPases, with a binding potency (Kb) of 7.7 μM for RalB-GDP. BQU57 can block its interaction with effector proteins (such as SEC5 and EXO84), inhibiting tumor cell migration, invasion and non-adherent growth. BQU57 downregulates the NF-κB signaling pathway, reduces the expression of IL-6, IL-8 and MMP-13, and inhibits apoptosis by regulating the Bcl-2/Bax balance. BQU57 also protects the extracellular matrix by inhibiting the Ral/NF-κB pathway and can be used for the study of degenerative diseases. BQU57 exhibits significant antitumor activity in triple-negative breast cancer (TNBC) models, inhibiting orthotopic tumor growth and lung metastasis and enhancing paclitaxel chemotherapy sensitivity .

Cat. No.	Product Name	Target	Research Area