Compounds with documented oncology research applications.
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Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
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CAS 212141-54-3
Vatalanib free base (PTK787 free base) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4.in vitro: Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC50 of 270 nM, 730 nM and 580 nM,…
CAS 924296-39-9
Inhibitor of ubiquitin-specific protease (USP) 7 activity (IC50 = 424 nM). Displays uncompetitive inhibition. Also inhibits USP7-mediated p53 deubiquitination (IC50 = 0.8 μM). Stabilizes p53 and inhibits cancer cell growth; induces p53-dependent apoptosis in…
CAS 1817626-54-2
PF06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), and used to treat diseases such as rheumatoid arthritis, lupus, and lymphomas.
CAS 2563855-03-6
K-975 is a first-in-class TEAD inhibitor, directly inhibiting YAP/TAZ-TEAD protein-protein interaction and showing a potent anti-tumor effect in malignant pleural mesothelioma. K-975 was covalently bound to an internal cysteine residue located in the…
CAS 209783-80-2
Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively.
CAS 1533438-83-3
TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor…
CAS 2329719-65-3
BRD-810 is a potent and selective MCL1 inhibitor with Kd of 0.3 nM (SPR) and IC50 of 0.4 nM (MCL1-Noxa HTRF), respectively. BRD-810 is a rapidly cleared inhibitor of MCL1 that has robust antitumor efficacy in hematological and solid tumor cancer models.
CAS 2765081-21-6
RAS-IN-2 (Compound A122) is a potent RAS(ON)MULTI inhibitor and can be used for the research of cancer.
CAS 218791-21-0
M40403 is a small molecule, synthetic manganese containing superoxide dismutase mimetic (SODm) that removes superoxide anions without interfering with other reactive species known to be involved in inflammatory responses (e.g. nitric oxide, NO and…
CAS 1703793-34-3
Avapritinib is a potent and selective exon 17 mutant KIT kinase inhibitor with IC50 of 0.27 nM for KIT D816V.
CAS 1334298-90-6
Itacitinib is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis.
CAS 1599440-13-7
Deruxtecan, a topoisomerase I inhibitor, is an exatecan derivative (DX-8951 derivative) with a cleavable pepetide linker and a maleimide group. The maleimide group in Deruxtecan can react with antibody to form antibody-drug conguates (ADC) such as Trastuzumab…
CAS 155514-72-0
IRES-J007 ia an improved IRES inhibitor that blocks IRES-hnRNP A1 binding; binds to a small pocket structure within the RRM-containing fragment of hnRNP A1 (UP1 fragment), inhibits cyclin D1 and c-MYC IRES activity to a greater extent compared with C11…
CAS 163515-35-3
Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker.
CAS 1197160-78-3
Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. PKI-587 is equally effective in both complexes of mTOR, mTORC1 and mTORC2.
CAS 942183-80-4
SCH772984 potently inhibits ERK1 and ERK2 activity with IC50s of 4 and 1 nM, respectively.
CAS 2454676-05-0
Benitrobenrazide is a novel selective hexokinase 2 (HK2) inhibitor, blocking cancer cells growth by targeting glycolysis.
CAS 1853279-29-4
ZB716 is a steroidal, orally bioavailable SERD (selective estrogen receptor downregulator) that binds to ER with high affinity and exerts its antiestrogenic effect on ER-expressing breast cancer cells.
CAS 186692-46-6
Roscovitine is a potent and selective CDKs inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.
CAS 202350-68-3
PNU-159682, a highly potent metabolite of the anthracycline nemorubicin with outstanding cytotoxicity, is a potent ADCs cytotoxin.
CAS 780757-88-2
ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. It works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM.
CAS 2460249-19-6
PF-07104091 is an orally bioavailable inhibitor of cyclin-dependent kinase 2 (CDK2), with potential antineoplastic activity. Upon administration, CDK2 inhibitor PF-07104091 selectively targets, binds to and inhibits the activity of CDK2. This may lead to cell…
CAS 606143-52-6
Selumetinib is a highly potent MEK inhibitor, with an IC50 of 14 nM against MEK1.
CAS 110078-46-1
Plerixafor is a selective CXCR4 antagonist with an IC50 of 44 nM.
CAS 1341200-45-0
TP-0903 is a potent and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM.
CAS 2105904-82-1
AB-680 is highly potent, reversible and selective small molecule inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity[1].
CAS 851688-13-6
IMTPPE (SID 3712502) is a novel small molecule capable of inhibiting androgen receptor (AR) transcriptional activity (IC50=1 uM) and protein level in C4-2 prostate cancer cells; IMTPPE inhibited proliferation of AR-positive, but not AR-negative, prostate…
CAS 125317-39-7
Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
CAS 510-30-5
Echinocystic acid a pentacyclic triterpene isolated from the fruits of Gleditsia sinensis Lam, has potent antioxidant, anti-inflammatory and anti-tumor properties. In vitro: Echinocystic acid (EA) inhibit the formation of osteoclast. EA inhibit RANKL-induced…
CAS 2734853-80-4
Fludarabine-Cl has inhibition effect on RNA adenosine deaminase 1(ADAR1), and can be used for preventing and/or treating cancer or tumor-related diseases[1].
CAS 2621928-55-8
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRASG12D of 0.2 pM. MRTX1133…
CAS 131068-23-0
Hydrazinocurcumin is a synthetic curcumin derivative that inhibits the proliferation of bovine aortic endothelial cells (BAECs) with IC50 of 520 nM without cytotoxicity, inhibits STAT3 phosphorylation and downregulates an array of STAT3 downstream targets;…
CAS 1809336-93-3
Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma.
CAS 2684216-48-4
Gly3-VC-PAB-MMAE consists a cleavable ADC linker (Gly3-VC-PAB) and a potent tubulin inhibitor (MMAE). Gly3-VC-PAB-MMAE can be used in the synthesis of antibody-drug conjugates (ADCs).
CAS 833481-73-5
2OH-BNPP1 is an inhibitor of BUB1 kinase, a Ser/Thr kinase, used for the treatment of cancer.
CAS 2126737-28-6
SB02024 is a novel highly potent, selective, ATP competitive, orally active inhibitor of vacuolar protein sorting 34 (Vps34) with Kd of 1 nM, >1000 times selective towards other PI3K isoenzymes; SB02024 is also highly selective at 1 uM in the DiscoveRx…
CAS 878385-84-3
AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.
CAS 1402608-02-9
BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.
CAS 2407860-35-7
ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer.
CAS 2138861-99-9
ABBV-744 is a highly BDII-selective BET bromodomain inhibitor, used in the research of inflammatory diseases, cancer, and AIDS.
CAS 1399840-35-7
MTDIA, also known as MT-DADMe-ImmA, and Methylthio-DADMe-Immucillin A, is a MTAP inhibitor. Human 5'-methylthioadenosine phosphorylase (MTAP) is solely responsible for 5'-methylthioadenosine (MTA) metabolism to permit S-adenosylmethionine salvage.…
CAS 497061-48-0
DC_AC50 is a dual inhibitor of Atox1 and CCS (copper chaperones). Inhibiting intracellular copper chaperones as a means of reducing/preventing acquired chemotherapy resistance[1].
CAS 112093-28-4
Endoxifen Z-isomer is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen inhibits hERG tail currents at 50 mV in a…
CAS 283173-50-2
Rucaparib is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, and also shows binding affinity to eight other PARP domains.
CAS 229971-81-7
Exherin, also known as ADH-1, is a small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities. ADH-1 selectively and competitively binds to and blocks N-cadherin, which may result in disruption of tumor…
CAS 2937344-16-4
BI-2493 is a structural analogue of BI-2865 and a highly selective pan-KRAS inhibitor. BI-2493 can attenuate tumor growth. BI-2493 can be used for cancer iseases research.
