Cancer Targeted Therapy

SHP099 hydrochloride is a potent, selective and orally available SHP2 inhibitor with an IC₅₀ of 70 nM.

Methylprednisolone succinate (Methylprednisolone hydrogen succinate) sodium is a prodrug of Methylprednisolone (HY-B0260) and glucocorticoid with immunosuppressant and anti-inflammatory activity. Methylprednisolone succinate sodium binds cytosolic glucocorticoid receptors, translocates to nuclei, and modulates target gene transcription. Methylprednisolone succinate sodium alters Bax, Bcl-2, occludin, and ZO-1 expression; attenuates TLR4/NF-κB signaling; suppresses proinflammatory cytokine production and immune cell activation. Methylprednisolone succinate sodium can be used for the research of intracranial haemorrhage, rheumatoid arthritis, multiple sclerosis, preterminal cancer, inflammatory conditions, shock, immediate-type hypersensitivity, acute myocardial ischemia, hypoxic heart muscle damage, and traumatic spinal cord injury.

Dapagliflozin ((2S)-1,2-propanediol, hydrate) is the S-enantiomer of Dapagliflozin 1,2-propanediol, hydrate. Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine. Dapagliflozin ((2S)-1,2-propanediol, hydrate) induces HIF1 expression and attenuates renal IR injury.

ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with IC₅₀ value of 100 nM.

Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC₅₀ values of 23 and 29 nM for recombinant BRaf^V600E and EGFR, respectively.

YTHDC1-IN-1 is a selective YTHDC1 inhibitor with a K_d of 49 nM and an IC₅₀ of 0.35 μM. YTHDC1-IN-1 can inhibit the proliferation and induce apoptosis of acute myeloid leukemia cell lines. YTHDC1-IN-1 has anti-tumor activity.

NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC₅₀ values of <30 nM for both p300/CBP and BET bromodomains. NEO2734 is active in SPOP mutant and wild-type prostate cancer.

NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC₅₀ for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 inhibits NSD2 (IC₅₀ of 170 nM) through a direct interaction with the catalytic SET domain (K_d of 370 nM).

JNK-IN-7 is a potent JNK inhibitor with IC₅₀ of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, respectively.

Clorgyline (M&B 9302) is a selective, irreversible monoamine oxidase A (MAO-A) inhibitor that can cross the blood-brain barrier and exhibits activity against the 5-HT Receptor at very high doses. Clorgyline regulates monoamine neurotransmitter levels, the release of dopamine and acetylcholine, the uptake and effects of Tyramine (HY-W007606), noradrenergic function, circadian locomotor activity rhythms, feeding behavior, and body weight. Clorgyline induces tumor-suppressive transcriptional programs, secretory differentiation, androgen signaling regulation, Bcl-2 expression, and radioprotective effects in non-malignant cells. Clorgyline is used in the research of high-grade prostate cancer, Huntington's disease, major affective disorder, radiation-induced normal tissue toxicity, and obesity.

PD176252 is a potent antagonist of neuromedin-B preferring (BB₁) and gastrin-releasing peptide-preferring (BB₂) receptor with K_is of 0.17 nM and 1 nM for human BB₁ and BB₂ receptors, and 0.66 nM, 16 nM for Rat BB₁ and BB₂ receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC₅₀s of 0.31 and 0.66 μM in HL-60 cells.

A1874 is an orally active BRD4 PROTAC degrader with a DC₅₀ of 32 nM. A1874 degrades BRD4 via the ubiquitin-proteasome system by recruiting the MDM2 E3 ligase, while disrupting the MDM2-p53 interaction to stabilize p53 and upregulate p21, thereby inducing cell cycle arrest and apoptosis. A1874 exhibits selectivity for wild-type p53 cells and MDM2-amplified tumors, and it can be used in research on breast cancer, colorectal cancer, melanoma, lung cancer, lymphoma, myeloid leukemia, osteosarcoma, and glioblastoma.

Enzomenib (DSP-5336) is an orally active Menin inhibitor (IC₅₀=1.4 nM, K_d=6.0 nM). Enzomenib disrupts the interaction between Menin and KMT2A/MLL fusion proteins, specifically inhibits the expression of leukemia driver genes such as HOX/MEIS1, and upregulates ITGAM. Enzomenib effectively induces cell differentiation, inhibits tumor cell proliferation, and suppresses primitive cell colony formation. Enzomenib reduces disease burden and prolongs survival, but causes adverse reactions including differentiation syndrome and QTc interval prolongation. Enzomenib is used for research on relapsed/refractory acute myeloid leukemia, acute lymphoblastic leukemia, and other hematologic malignancies with mixed lineage leukemia (MLL) rearrangements or NPM1 mutations.

Ivuxolimab is a fully human IgG2 agonist targeting OX40 (CD134), which selectively binds to the OX40 receptor on the surface of activated CD4⁺ and CD8⁺ T cells without inducing antibody-dependent cytotoxicity. Ivuxolimab can promote T cell proliferation, survival and cytokine (such as IFN-γ, IL-2) secretion, inhibit regulatory T cell function, and enhance anti-tumor immune response. Ivuxolimab can be used in the study of melanoma, hepatocellular carcinoma, head and neck squamous cell carcinoma, etc.

CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC₅₀ of 1.7 nM for TTK in vitro. CFI-402257 hydrochloride has anti-cancer activity.

Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC₅₀s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer.

ABD957 is a potent and selective covalent inhibitor of the ABHD17 family of depalmitoylases, with an IC₅₀ of 0.21 μM for ABHD17B. ABD957 can block N-Ras signaling and the growth of NRAS-mutant AML cells.

Anamorelin (RC-1291) hydrochloride is an orally active Ghrelin receptor agonist with an EC₅₀ of 0.74 nM. Anamorelin hydrochloride can promote appetite, increase body weight, and stimulate the secretion of growth hormone and insulin-like growth factor-1. Anamorelin hydrochloride can be used in the research of anorexia and cancer cachexia.

Ginisortamab (UCB6114) is a fully human IgG4P anti Gremlin-1 monoclonal antibody, with mean IC₅₀ values of 8.2 nM and 9 nM against human and mouse gremlin-1, respectivly. Ginisortamab inhibits gremlin-1 antagonism of BMP signaling pathways. Ginisortamab has the potential for the research of gastrointestinal (GI) tumors.

Pepinemab (VX 15/2503) is a human monoclonal antibody against SEMA4D, a signalling protein 4D (SEMA4D), also known as CD100, which is a regulator of neuronal development and plays a role in a variety of cellular processes. Pepinemab can be used in the study of various neurodegenerative diseases such as Alzheimer's disease by blocking the activity of SEMA4D.