oral activity

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6 22 90 15 20 20 57 58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7 0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.

Pexidartinib (PLX-3397) is a capsule containing a small-molecule receptor tyrosine kinase (RTK) inhibitor targeting KIT, CSF1R, and FLT3, with potential antineoplastic activity.

Onvansertib (NMS-1286937) is a PLK1 inhibitor (IC50=2 nM) with high selectivity and oral activity. Onvansertib has antitumor activity and inhibits tumor growth.

Doxycycline (Doxiciclina) belongs to the tetracycline class of antibiotics and is a broad-spectrum metalloproteinase (MMP) inhibitor with oral activity. Doxycycline has antibacterial activity and antitumor activity.

Paquinimod (ABR 25757) is a S100A9 inhibitor preventing S100A9 binding to TLR-4.

Denifanstat (FASN-IN-2) is a fatty acid synthase (FASN) inhibitor (IC50=0.052 μM, EC50=0.072 μM) with selective and oral activity. Denifanstat has been used in studies of steatohepatitis.

Navitoclax (ABT-263) is a potent oral Bcl-2 inhibitor that binds to Bcl-xL, Bcl-2, and Bcl-w proteins (Ki<1 nM), demonstrating antitumor activity and inducing apoptosis.

Leupeptin hemisulfate is a protease inhibitor with cell membrane-permeable, reversible, competitive, and oral activities. Leupeptin hemisulfate inhibits the activity of Cathepsin B, Cathepsin H, and Cathepsin L, and blocks fusion of amphipathic lysosomes. Leupeptin hemisulfate also has anti-inflammatory activity.

Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.

PLX5622 is a highly selective, brain-penetrant, and orally active CSF1R inhibitor.

PF-07321332 is a potent and orally active inhibitor of SARS-CoV 3C-like protease (3CLPRO) .

VT104 is a potent YAP TAZ inhibitor with oral activity that can be used in cancer research. VT104 prevents palmitylation of endogenous TEAD1 and TEAD3 proteins.

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4 5.2 nM). Lenvatinib has strong anti-tumor activity.

Finerenone (BAY-948862) is a nonsteroidal antagonist of the mineralocorticoid receptor (MR) (IC50=18 nM) with selective and oral activity. Finerenone is used in the treatment of patients with chronic kidney disease with type 2 diabetes.

Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

Capivasertib (AZD5363) is a broad-spectrum AKT inhibitor with inhibitory activity against Akt1, Akt2, and Akt3 (IC50=3 7 7 nM) with oral activity. Capivasertib has antitumor activity for the treatment of breast cancer.

CSN5i-3 is a novel potent oral and selective CSN5/Jab1 inhibitor that inhibits CSN-catalyzed Cul1 deneddylation with an IC50 value of 5.8 nM.CSN5i-3 exhibits anticancer activity, inhibits cell proliferation and induces apoptosis in human breast cancer cells.

Ceralasertib (AZD6738) is an orally active, selective ATR kinase inhibitor with an IC50 of 1 nM.

Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity, inhibiting PI3Kβ γ δ with low activity (IC50=250 290 1200 nM). Alpelisib demonstrates antitumor activity and specifically targets PIK3CA mutant tumors.

Gilteritinib (ASP2215) is a potent inhibitor of FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preclinical studies, gilteritinib demonstrated strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 clinical trials for acute myeloid leukemia.

4-Hydroxytamoxifen (ICI 79280) is the active metabolite of Tamoxifen, an estrogen receptor modulator (SERM) with selective and oral potency. 4-Hydroxytamoxifen has antitumor activity and may be used in breast cancer research.

Selinexor (KPT-330) is a small molecule inhibitor of CRM1 with selective and oral activity. Selinexor blocks the cell cycle, induces apoptosis, and has antitumor activity for the treatment of multiple myeloma.

Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy. Temozolomide is stable under acidic conditions and hydrolyzes under neutral or slightly alkaline conditions.

SAR-114137 is an inhibitor of cysteine cathepsin with oral activity.

Lidorestat (IDD-676) is an aldose reductase inhibitor (IC50: 5 nM) with effective, selective and oral activity. Lidorestat improves nerve conduction and reduces the formation of cataracts. Lidorestat can be used to treat complications of chronic diabetes.

SKLB 1028 (Ruserontinib) is a new type of oral multikinase inhibitor of EGFR, FLT3, and Abl. SKLB 1028 shows excellent activity in FLT3-driven AML models and considerable potency in CML models containing Abl mutants.

Cot inhibitor-2 is a cot (Tpl2/MAP3K8) inhibitor (IC50: 1.6 nM) with potency, selectivity and oral activity. cot inhibitor-2 inhibits LPS-stimulated TNF-α production in human whole blood with an IC50 of 0.3 μM.

Nolomirole HCl (CHF 1035) is a novel selective dopamine agonist with oral activity and inhibitory effects on norepinephrine release, which can be used to study mild chronic heart failure.

RO5263397 is a TAAR1 specific agonist with oral activity that has been used in antidepressant studies. It has also been found to act as an inhibitor of the enzyme cyclooxygenase-2 (COX-2), which is involved in the synthesis of prostaglandins.

IHMT-MST1-58 is a STE20-like protein 1 kinase (MST1) inhibitor (IC50:23 nM) with high efficiency, selectivity and oral activity. IHMT-MST1-58 can be used to study type 1 or type 2 diabetes.

Pulrodemstat (CC-90011) is a highly potent and selective inhibitor of lysine specific demethylase-1 (LSD1), exhibiting a reversible mode of action and oral bioavailability. With an impressive IC50 of 0.25 nM, Pulrodemstat effectively suppresses LSD1 enzymatic activity while demonstrating minimal inhibition of LSD2, MOA-A, and MAO-B enzymes. Additionally, Pulrodemstat possesses remarkable anticancer properties, promoting differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells.

Seridopidine (ACR343) is a modulator of dopaminergic activity that is used as an oral therapy for schizophrenia, Parkinson's disease, and Tourette's syndrome.

BTA-9881 is a novel RSV fusion inhibitor with oral activity and antiviral activity for the study of respiratory syncytial virus infections.

Bisubstrate Inhibitor 78 HCl is an NNMT inhibitor (IC50 = 1.41 μM) with potential anticancer activity, inhibiting the proliferation of HSC-2 oral cancer cells at 100 μM.

Tenofovir amibufenamide (HS-10234) is a Tenofovir prodrug, an antiviral compound with oral activity. Tenofovir amibufenamide inhibits hepatitis B virus (HBV) and can be used in chronic hepatitis B (CHB) studies.

Dimethyl fumarate (DMF) is an Nrf2 activator with oral activity and blood-brain barrier permeability. Dimethyl fumarate has antimicrobial, anti-inflammatory, and immunomodulatory activities and has been used in the study of multiple sclerosis.

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.

Nystatin (Fungicidin) is a topical and oral antifungal agent with activity against many species of yeast and candida albicans, which is used largely to treat skin and oropharyngeal candidiasis.

Oseltamivir phosphate (GS 4104) is a neuraminidase (NA) inhibitor with oral activity. Oseltamivir phosphate has antiviral activity and is effective against a wide range of influenza viruses, inhibiting mature influenza viruses from breaking away from host cells.

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6 20 22 nM for Raf-1 VEGFR-3 B-Raf).

Imatinib Mesylate (STI-571) is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively).

Doxifluridine (AMC 0101) is a fluoropyrimidine derivative and oral prodrug of the antineoplastic agent 5-fluorouracil (5-FU) with antitumor activity. Doxifluridine, designed to circumvent the rapid degradation of 5-FU by dihydropyrimidine dehydrogenase in the gut wall, is converted into 5-FU in the presence of pyrimidine nucleoside phosphorylase. 5-FU interferes with DNA synthesis and subsequent cell division by reducing normal thymidine production and interferes with RNA transcription by competing with uridine triphosphate for incorporation into the RNA strand.

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

Osimertinib mesylate (AZD-9291 mesylate) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib mesylate has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

Baricitinib (INCB028050) is a JAK1 and JAK2 inhibitor (IC50=5.9 5.7 nM) with selective and oral activity. Baricitinib has potential anti-inflammatory, immunomodulatory and anti-tumor activity.

Ribociclib (LEE011) is an orally available, and highly specific CDK4 6 inhibitor (IC50：10 39 nM).

Quinidine sulfate dihydrate (Pitayine Sodium) is a potent and selective cytochrome P450db inhibitor