Bioactive molecules

CAT # Product Name Description
CPD100464 Erdafitinib Erdafitinib, also known as JNJ-42756493, is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Upon oral administration, JNJ-42756493 binds to and inhibits FGFR, which may result in the inhibition of FGFR-related signal transduction pathways and thus the inhibition of tumor cell proliferation and tumor cell death in FGFR-overexpressing tumor cells. FGFR, upregulated in many tumor cell types, is a receptor tyrosine kinase essential to tumor cell proliferation, differentiation and survival.
CPD100391 SHP394
CPD100390 SHP389 (free base)
CPD10000 BI-3406 BI-3406 is Potent & Selective SOS1::KRAS Inhibitor (IC50=5 nM), which Opens a New Approach for Treating KRAS-Driven Tumours. BI 3406 selectively binds to SOS1 and blocks the interaction with KRAS, irrespective of the KRAS mutation. BI 3406 causes RAS GTP and pERK reduction and inhibits cell growth of KRAS mutated cell lines, carrying most of the typical KRAS mutations (i.e. G12D, G12V, G13D and others). BI 3406, when administered orally to tumour bearing mice, causes a dose dependent tumour static effect that can be converted into regressions when combined with MEK1 inhibition
CPD3242 RMC-4550 RMC-4550 is a potent and selective SHP2 inhibitor. RMC-4550 identified as a high quality tool compound to study the role of SHP2 in tumor biology, both in vitro and in vivo in rodents. SHP2 is a convergent signalling node and inhibition of SHP2 is effective in targeting both upstream (RTK-driven) and downstream (RAS-GTP dependent) mutations in the RAS-MAPK pathway
CPD2806 BI-167107 BI-167107 is a β-Arrestin-Biased D2R Agonist. Targeting the D2R mediated activation of β-arrestin-2 might therefore be a valuable approach for the design of novel antiparkinsonian drugs.
CPD3611 SB-204990 SB-204990 is the prodrug of the potent ATP citrate-lyase inhibitor SB-201076. SB-204990, when administered orally to rats, was absorbed into the systemic circulation, pharmacologically relevant concentrations of SB-201076 were recovered in the liver. SB-204990 (25 mg/kg per day) also decreased plasma cholesterol levels (by up to 23%) and triglyceride levels (by up to 38%) in the dog, preferentially decreasing low-density lipoprotein compared with high-density lipoprotein cholesterol levels. SB-204990 is an important enzyme in controlling substrate supply for lipid synthesis de novo and a potential enzyme target for hypolipidaemic intervention.
CPD3619 CPD3619
CPD3236 CPD3236
CPD3235 CPD3235
CPD3234 BAY-545 BAY-545 is a potent and selective antagonist of the A2B adenosine receptor
CPD3232 NTN21277 NTN21277, also known as Gefitinib-based PROTAC 3 is a VHL-recruiting PROTAC that induces the degradation of EGFR and EGFR mutants with DC50 of 11.7 nM and 22.3 nM for HCC827 cell (Exon 19 del) and H3255 cell (L858R).
CPD3233 AZD-3409 AZD-3409 is a potent prenyl transferase inhibitor. AZD-3409 showed higher potency than lonafarnib. The mean IC(50) for cytotoxicity of AZD3409 was 510 in MEF cells, 10,600 in A549 cells and 6,170 in MCF7 cells, respectively. In these cells, the IC(50) for FTase activity of AZD3409 ranged from 3.0 to 14.2 nM and of lonafarnib from 0.26 to 31.3 nM. AZD3409 inhibits farnesylation to a higher extent than geranylgeranylation. Both inhibition of farnesylation and geranylgeranylation could not be correlated to the antiproliferative activity of the drug. AZD3409 might be active in gefitinib-resistant breast carcinoma.
CPD3219 EW-7197 Hydrochloride EW-7197 Hydrochloride is a highly potent, selective, and orally bioavailable inhibitor of TGF-β type 1 receptor kinase.
CPD3218 BMS-955176 GSK3532795, also known as BMS-955176, is a potent, orally active, second-generation HIV-1 maturation inhibitor (MI) that advanced through phase IIb clinical trials. GSK3532795 combines broad coverage of polymorphic viruses (EC50 <15 nM toward a panel of common polymorphisms representative of 96.5% HIV-1 subtype B virus) with a favorable pharmacokinetic profile in preclinical species.
CPD3618 TAS-120 TAS-120 is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. FGFR inhibitor TAS-120 selectively and irreversibly binds to and inhibits FGFR, which may result in the inhibition of both the FGFR-mediated signal transduction pathway and tumor cell proliferation, and increased cell death in FGFR-overexpressing tumor cells. FGFR is a receptor tyrosine kinase essential to tumor cell proliferation, differentiation and survival and its expression is upregulated in many tumor cell types.
CPD1609 SB-423562 SB-423562 is a calcium-sensing receptor antagonist potentially for the treatment of autosomal dominant hypocalcemia
CPD3616 CPD3616
CPD3508 GSK547 GSK547 is a highly selective and potent inhibitor of RIP1 kinase that targets RIP1 in vivo
CPD2801 OSI-027 OSI-027 is an orally bioavailable mammalian target of rapamycin (mTOR) kinase inhibitor with potential antineoplastic activity. mTOR kinase inhibitor OSI-027 binds to and inhibits both the raptor-mTOR (TOR complex 1 or TORC1) and the rictor-mTOR (TOR complex 2 or TORC2) complexes of mTOR, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. mTOR is a serine/threonine kinase that is upregulated in some tumors and plays an important role downstream in the PI3K/Akt/mTOR signaling pathway. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
CPD3504 BAY-218
CPD2807 BAY-293 BAY-293 is a potent SOS1 inhibitor that blocks RAS activation via disruption of the RAS-SOS1 interaction. BAY-293) selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM and is a valuable chemical probe for future investigations.
CPD2809 CPD2809 AMG-510 is a potent KRAS G12C covalent inhibitor. AMG-510 selectively targets the KRAS p.G12C mutant, at either the DNA, RNA or protein level, and prevents, through an as of yet not elucidated manner, expression of and/or tumor cell signaling through the KRAS p.G12C mutant. This may inhibit growth in KRAS p.G12C-expressing tumor cells

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