Active Pharmaceutical Ingredients

Catalog No. Product Name Information
S6676 Ebselen Ebselen (DR 3305, SPI-1005, PZ-51, CCG-39161) is a small-molecule capsid inhibitor of HIV-1 Replication with IC50 of 46.1 nM in TR-FRET assay.
S8018 Nirogacestat (PF-03084014) Nirogacestat (PF-03084014, PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay. Nirogacestat (PF-03084014, PF-3084014) induces apoptosis. Phase 2.
S1060 Olaparib (AZD2281) Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.
S8724 Lazertinib Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.
S1300 Tegafur (FT-207) Tegafur (NSC 148958,Fluorafur,FT-207) is a substance being used in the treatment of some types of cancer.
S7028 Duvelisib (IPI-145) Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3.
S1044 Temsirolimus Temsirolimus is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.
S6659 Rimegepant (BMS-927711) Rimegepant (BMS-927711, BHV-3000) is a potent, selective, competitive human calcitonin gene-related peptide (CGRP) receptor antagonist with ki of 0.027 nM.
S6663 Resmetirom (MGL-3196) Resmetirom (MGL-3196, VIA-3196) is a liver-directed, orally active, selective thyroid hormone receptor β(THR-β) agonist with an EC50 of 0.21 μM,shows 28-fold selective for THR-β over THR-α in a functional assay.
S8873 Letermovir (AIC246) Letermovir (AIC246, MK-8228) is a novel anti-CMV compound which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
S2183 Infigratinib (BGJ398) Infigratinib (BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.
S7252 Selinexor (KPT-330) Selinexor (KPT-330, ATG-010) is an orally bioavailable selective CRM1 inhibitor. Phase 2.
S1119 Cabozantinib (XL184) Cabozantinib (XL184) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.
S2727 Dacomitinib Dacomitinib is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay. Dacomitinib inhibits ERBB2 and ERBB4 with IC50 of 45.7 nM and 73.7 nM, respectively. Dacomitinib is effective against NSCLCs with EGFR or ERBB2 mutations as well as those harboring the EGFR T790M mutation. Dacomitinib inhibits cell growth and induces apoptosis. Phase 2.
S8781 Selpercatinib (LOXO-292) Selpercatinib (LOXO-292, ARRY-192) is a potent and specific RET (c-RET) inhibitor with IC50 values of 1 nM, 2 nM, 2 nM, 4 nM, 2 nM, 2 nM for WT RET, RET V804M, RET V804L, RET A883F, RET M918T and RET S891A respectively.
S2071 Prulifloxacin (NM441) Prulifloxacin (NM441, AF 3013), the prodrug of ulifloxacin, is a broad-spectrum oral fluoroquinolone antibacterial agent.
S2151 Sonidegib Sonidegib is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.
S7007 Binimetinib (MEK162) Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Binimetinib induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy. Phase 3.
S1267 Vemurafenib (PLX4032) Vemurafenib (PLX4032, RG7204, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.
S2001 Elvitegravir Elvitegravir is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.