Showing 1137–1152 of 5741 results

SGC707

SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.

CB1954

CB1954(Tretazicar) is a anticancer prodrug that is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent. It can be activated by NAD(P)H quinone oxidoreductase 2.

Licochalcone A

Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.

4-Hydroxytamoxifen

4-Hydroxytamoxifen is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. It activates on-target modification frequency for intein-Cas9 variants.

Nazartinib (EGF816, NVS-816)

Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro.

EPZ020411 2HCl

EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.

BLU9931

BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with IC50 of 3 nM, about 297-, 184-, and 50-fold selectivity over FGFR1/2/3, respectively.

Pexidartinib (PLX3397)

Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Phase 3.

MI-503

MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM. It shows pronounced growth suppressive activity in a panel of human MLL leukemia cell lines(GI50 at 250 nM-570 nM range), but only a minimal effect in human leukemia cell lines without MLL translocations.

MI-463

MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM.

MI-136

MI-136 can specifically inhibit the menin-MLL interaction. It inhibits DHT-induced expression of androgen receptor (AR) target genes.

AI-10-49

AI-10-49 is a selective inhibitor of the binding of CBFβ-SMMHC to RUNX1 with IC50 of 260 nM.

AMG319

AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.

Itacitinib (INCB39110)

Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.

MHY1485

MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.

Afatinib (BIBW2992) Dimaleate

Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.