| DC74646 |
EB-PSMA-617 |
EB-PSMA-617 is an Evans blue-modified prostate-specific membrane antigen (PSMA) 617 ligand for making 177Lu-EB-PSMA, which is potential useful for Metastatic Castration-Resistant Prostate Cancer. |
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| DC74647 |
Neladalkib |
Neladalkib, also known as NVL-655, and NUV-655, is a selective, brain-penetrant ALK inhibitor with antitumor activity against the lorlatinib-resistant G1202R/L1196M compound mutation. NUV-655 (NVL-655) inhibited the kinase activity of ALK and ALK G1202R/L1196M with Kiapp < 5 nM in the presence of 1 mM ATP and with selectivity over TRKB. Across a panel of 335 wild-type kinases, NUV-655 (NVL-655) inhibited only 5 other kinases by >50% within 10-fold of its IC50 for ALK. NUV-655 (NVL-655) also selectively inhibited ALK in cells. It inhibited the growth of Ba/F3 cells driven by expression of EML4-ALK variant 1 (v1) with either wild-type kinase domain or drug-resistance mutations G1202R, G1202R/L1196M, or G1202R/G1269A at IC50 values < 10 nM and with selectivity over TRKB. In vivo, NUV-655 (NVL-655) induced regression at well-tolerated doses in a Ba/F3 EML4-ALKv1 G1202R/L1196M xenograft model. Furthermore, NUV-655 (NVL-655) demonstrated brain penetrance in rodent pharmacokinetic studies. |
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| DC74648 |
Demethyleneberberine chloride |
Demethyleneberberine, a berberine metabolite, is a mitochondria-targeted antioxidant isolated from Cortex Phellodendri chinensis that exhibits multiple pharmacological activities including anti-microbial, anti-inflammatory, anti-diarrhea and anti-cancer. |
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| DC74649 |
NOTA-TATE |
DOTA-TATE can be reacted with the radionuclides gallium-68 (T1/2 = 68 min), lutetium-177 (T1/2 = 6.65 d) and copper-64 (T1/2 = 12.7 h) to form radiopharmaceuticals for positron emission tomography (PET) imaging or radionuclide therapy. DOTA-TATE is a compound containing tyrosine3-octreotate, an SSR agonist, and the bifunctional chelator DOTA (tetraxetan). SSRs are found with high density in numerous malignancies, including CNS, breast, lung, and lymphatics. |
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| DC74650 |
NOTA-NFB |
NOTA-NFB is a ligand for making radioactive complex 68Ga-NOTA-NFB, which is am imaging agent and a tracer for CXCR4 evaluation in glioma patients after measuring the dosimetry of 68Ga-NOTA-NFB in healthy volunteers. |
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| DC74651 |
Alfatide II |
Alfatide II is ligand for making 18F-Alfatide II PET/CT for Identification of Breast Cancer: A Preliminary Clinical Study. 18F-alfatide II has been proven to have excellent clinical translational potential. |
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| DC74652 |
DOTA-c(RGDyK) |
DOTA-c(RGDyK) is useful ligand for making 225Ac-DOTA-c(RGDyK), which is a potential radiopharmaceutical for targeted alpha particle therapy. |
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| DC74653 |
Caspase-1 Inhibitor IV |
Caspase-1 Inhibitor IV controls the biological activity of Caspase-1. This small molecule/inhibitor is primarily used for Cancer applications. |
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| DC74654 |
NOTA-E(cRGDfK)2 |
NOTA-E(cRGDfK)2 is a ligand to making 68Ga-DOTA-E[c(RGDfK)]2, which is a PET Imaging agent of SHARPIN-Regulated Integrin Activity. E[c(RGDfk)]2 = glutamic acid-[cyclo(arginyl-glycyl-aspartic acid-D-phenylalanine-lysine). |
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| DC74655 |
NOTA-P2-RM26 |
NOTA-P2-RM26 is a high-affinity NOTA-conjugated bombesin antagonist for GRPR-targeted tumor imaging |
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| DC74656 |
NOTA-cyclic RGDyK |
NOTA-cyclic RGDyK is a ligand to bind 68Ga for molecular imaging of αvβ3 integrin overexpressing tumor. |
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| DC74657 |
NVP-CGM097 free base |
NVP-CGM097 is a potent and selective MDM2 inhibitor. P53 wild type GOT1 cells were sensitive to NVP-CGM097, p53mutated BON1 and p53mutated NCI-H727 cells were resistant to NVP-CGM097. Incubation of GOT1 cells with NVP-CGM097 at 100, 500, and 2,500 nM for 96 h caused a significant decline in cell viability to 84.9 ± 9.2% (p < 0.05), 77.4 ± 6.6% (p < 0.01), and 47.7 ± 9.2% (p < 0.01). NVP-CGM097 can inhibit the proliferation of tumor cells. NVP-CGM097 could reverse ABCB1-mediated MDR by directly blocking the ABCB1-mediated drug efflux and raising the accumulation of chemotherapeutic drugs in cancer cells. NVP-CGM097 tended to bind to the inhibitory site, which led to slight but critical conformational changes in the transporter and reduced the ATPase activity. |
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| DC74658 |
NOTA-JR-11 |
NOTA-JR-11 is a somatostatin receptor (SSTR) antagonist. |
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| DC74659 |
DOTA-LM3 |
DOTA-LM3 is a somatostatin receptor ( SSTR ) antagonist. |
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| DC74660 |
Monlunabant |
Monlunabant, also known as INV-202, is a potent CB1R inverse agonist. INV-202 demonstrated weight loss potential in a phase 1b trial and is currently in a phase 2 trial for diabetic kidney disease (DKD). INV-202 reduced glomerular injury, preserved podocyte structure and function, reduced injury to PTECs, and ultimately reduced renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model. |
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| DC74661 |
HEC96719 |
HEC96719 is a tricyclic farnesoid X receptor agonist (FXR agonist) for treatment of non-alcoholic steatohepatitis. HEC96719 exhibits excellent potency superior to GW4064 and obeticholic acid in in vitro and in vivo assays of FXR activation. It also shows higher FXR selectivity and more favorable tissue distribution dominantly in liver and intestine. Preclinical data on pharmacokinetic properties, efficacy, and safety profiles overall indicate that HEC96719 is a promising drug candidate for NASH treatment. |
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| DC74662 |
CHK1-IN-3 |
CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM. |
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| DC74663 |
DOTA |
DOTA is an azamacrocyle in which four nitrogen atoms at positions 1, 4, 7 and 10 of a twelve-membered ring are each substituted with a carboxymethyl group. It has a role as a chelator and a copper chelator. It derives from a hydride of a 1,4,7,10-tetraazacyclododecane. It is a a metal chelate in use in medical diagnostics. |
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| DC74664 |
BAL-0028 |
BAL-0028 (Compound 3) is a NLRP3 activation inhibitor with a IC50 value of 25 nM. |
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| DC74665 |
Protoporphyrin IX |
Protoporphyrin IX is an organic compound, classified as a porphyrin, that plays an important role in living organisms as a precursor to other critical compounds like heme (hemoglobin) and chlorophyll. It is a deeply colored solid that is not soluble in water. The name is often abbreviated as PPIX. Protoporphyrin IX florescence from 5-ALA administration is used in fluorescent-guided surgery of glioblastoma. Protoporphyrin IX is an important precursor for synthesis of verteporfin, an approved photosensitizer. |
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| DC74666 |
WJ-39 |
WJ-39 is an orally active aldose reductase (AR) inhibitor. |
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| DC74667 |
Hispolon |
Hispolon is a phenol originally isolated from I. hispidus that has diverse biological activities. |
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| DC74668 |
LMP744 free base |
LMP744, also known as Mj-III-65 and NSC-706744, is a DNA intercalator and topoisomerase inhibitor with antitumor activity. LMP744 produces persistent topoisomerase I cleavage complexes and overcome multidrug resistance. Consistent with Top1 poisoning, protein-linked DNA breaks were detected in cells treated with LMP744 at nanomolar concentrations. Studies in human cells in culture found LMP744 to be cytotoxic. Furthermore, limited cross-resistance was observed in camptothecin-resistant cell lines. LMP744 also exhibits antitumor activity in mouse tumor xenografts. |
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| DC74669 |
Rilpivirine HCl |
Rilpivirine, also known as TMC278, is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and reduced side-effect profile compared with older NNRTIs, such as efavirenz. Rilpivirine was approved for use in the United States in May 2011. |
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| DC74670 |
JTE-607 HCl |
JTE-607, also known as TO-207, is a cytokine production inhibitor potentially for the treatment of systemic inflammatory response, and induces apoptosis accompanied by an increase in p21waf1/cip1 in acute myelogenous leukemia cells. |
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| DC74671 |
CTP518 |
CTP518 is a HIV protease inhibitor and a deuterated Atazanivir derivative. |
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| DC74672 |
ZK-756326 dihydrochloride |
ZK-756326 is a potent, selective and non-peptide CCR8 chemokine receptor agonist. ZK 756326 inhibited the binding of the CCR8 ligand I-309 (CCL1), with an IC(50) value of 1.8 muM. ZK 756326 was a full agonist of CCR8, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1. |
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| DC74673 |
PRE-084 HCl |
PRE 084 is a high affinity selective sigma 1 agonist. |
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| DC74674 |
PF-05089771 |
PF-05089771 is a Selective Nav1.7 Inhibitor (IC50 = 11 nM) that interacts with the voltage-sensor domain (VSD) of domain IV. PF-05089771 exhibits a slow onset of block that is depolarization and concentration dependent, with a similarly slow recovery from block. Human hereditary gain- or loss-of-pain disorders have demonstrated an essential role of Nav1.7 sodium channels in the sensation of pain, thus making this channel an attractive target for new pain therapies. |
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| DC74675 |
Eliglustat tartrate |
Eliglustat, also known as Genz-112638, is is a potent and selective glucosylceramide synthase inhibitor. Eliglustat was approved for Gaucher's disease. Commonly used as the tartrate salt, the compound is believed to work by inhibition of glucosylceramide synthase. According to an article in Journal of the American Medical Association the oral substrate reduction therapy resulted in "significant improvements in spleen volume, hemoglobin level, liver volume, and platelet count" in untreated adults with Gaucher disease Type 1. |
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