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T4400 |
DIM-C-pPhOH
|
CDIM8 |
Apoptosis
,
Others
|
|
DIM-C-pPhOH (CDIM8) is a nur77 (NR4A1) antagonist,inhibits TGF-β induced cell migration of breast cancer cell lines,promotes ROS/endoplasmic reticulum stress and proapoptotic pathways in pancreatic cancer cell lines,mimi... |
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T23861 |
CAY10526
|
CAY-10526,BTH,CAY 10526 |
Prostaglandin Receptor
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CAY10526 (BTH) is a selective mPGES-1 inhibitor that acts as an inhibitor of the NF-κB signaling pathway. |
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T7698 |
BS194
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CDK
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BS194 is as a potent cyclin-dependent protein kinases (CDKs) inhibitor. |
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T15030 |
CycLuc1
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Others
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CycLuc1 is a brain penetrant luciferase substrate. CycLuc1 may be a superior BLI substrate as compared to D-luciferin for monitoring tumor growth of intracranial GBM xenografts. |
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T3469 |
PCI-27483
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PCI27483 |
Others
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PCI-27483 is an activated coagulation factor VIIa inhibitor with antithrombotic effects in a baboon model of arterial thrombosis. It also inhibits the growth of BxPC3 xenografts by 42% and 85% at doses of 60 and 90 mg/kg... |
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T33467 |
MOMIPP
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PI3K
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MOMIPP is a PIKfyve inhibitor and a macropinocytosis inducer. MOMIPP readily penetrates the blood-brain barrier and is moderately effective in suppressing progression of intracerebral glioblastoma xenografts[1][2]. |
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T2069L |
TH287 hydrochloride
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|
DNA/RNA Synthesis
,
MTH1
|
|
TH287 is a selective MTH1 inhibitor(IC50 : 0.8 nM). It causees incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses in patient-derived mouse xenografts. |
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T80725 |
ZK53
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Others
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ZK53 is a selective and potent activator of mitochondrial casein hydrolase protease P (HsClpP).ZK53 induces apoptosis and inhibits the hydrolysis of alpha-casein by HsClpP.ZK53 inhibits tumour growth in xenografts and na... |
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T71534L |
CIA-1 (Free base)
|
CIA-1(Free base） |
Gamma-secretase
|
|
CIA-1 (Free base) is a nuclear receptor COUP-TFII inhibitor with IC50 values ranging from 1.2 μM to 7.6 μM in prostate cancer cell lines. CIA-1 (Free base) inhibits tumor growth in a mouse model of prostate cancer xenogr... |
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T6695 |
Tasquinimod
|
ABR-215050 |
HDAC
|
|
Tasquinimod (ABR-215050) is a quinoline-3-carboxamide linomide analog with antiangiogenic and potential antineoplastic activities. Tasquinimod has been shown to decrease blood vessel density but the exact mechanism of ac... |
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T63049 |
CHD1Li 6.11
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Others
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|
CHD1Li 6.11 is a potent inhibitor of oncogenic CHD1L, acting on the cat-CHD1L recombinant protein (IC50: 3.3 μM). CHD1Li 6.11 is an orally active antitumour agent that significantly reduces the tumour volume of CRC xenog... |
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T6248 |
XL888
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HSP
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XL888 is an ATP-competitive inhibitor of Hsp90 ( IC50: 24 nM). Heat shock protein 90 (Hsp90) is a chaperone that maintains the functionality of client proteins involved in cell proliferation, cell cycling, and apoptosis.... |
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T21831 |
UCM05
|
G28UCM |
Fatty Acid Synthase
|
|
UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) with efficacy against HER2+ breast cancer xenografts, including in cell lines resistant to anti-HER2 drugs [1]. Additionally, it functions as an inhibito... |
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T3678 |
Entrectinib
|
RXDX-101,NMS-E628 |
Trk receptor
,
ROS
,
ALK
,
Autophagy
,
ROS Kinase
|
|
Entrectinib (RXDX-101) is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectini... |
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T28215 |
NT113
|
NT 113,NT-113 |
|
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NT113 is a pan-ERBB inhibitor with high brain penetrance. NT113 is active against GBM xenografts in which wild-type EGFR or EGFRvIII is highly expressed. NT113 inhibits the growth of glioblastoma xenografts with EGFR amp... |
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T34916 |
Transtinib
|
|
|
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Transtinib is an effective and irreversible EGFR tyrosine kinase inhibitor (EGFR-TKI) that is active against L858R/T790M mutated NSCLC cell lines and xenografts. |
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T71867 |
PKM2 inhibitor 2825-0090
|
|
|
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PKM2 inhibitor 2825-0090 is a Novel pyruvate kinase M2 (PKM2) inhibitor, reducing tumor growth of NSCLC xenografts in vivo. |
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T34166 |
PROTAC_ERRalpha
|
|
|
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PROTAC_ERRalpha is a proteolysis targeting chimeras (PROTAC) which provides broad tissue distribution and knockdown of the targeted ERRalpha protein in tumor xenografts. |
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T28203 |
NSC156529
|
NSC-156529,NSC 156529 |
|
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NSC156529 downregulates AKT1 signaling. NSC156529 efficiently decreases the proliferation of human cancer cells in vitro, and substantially inhibits the growth of prostate tumor xenografts in vivo. |
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T69479 |
CGC 11093
|
|
|
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CGC 11093 is a polyamine analog; inhibits growth of human prostate tumor xenografts in nude mice. It may prove useful in promoting regression of choroidal neovascularization. |
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T26441 |
A 74932
|
A74932,A-74932 |
|
|
A 74932 is a quinolone antibacterial agent and inhibitor of topoisomerase II enzyme. A-74932 possesses good activity in vivo against both systemic tumour, subcutaneously implanted murine solid tumours and human tumour xe... |
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T14340 |
Atiratecan
|
TP300 |
Others
|
|
Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models[1]. A... |
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T36674 |
DMU-212
|
|
Apoptosis
,
ERK
|
|
DMU-212 is a methylated derivative of Resveratrol , with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2... |
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T70151 |
MeTC7
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|
|
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MeTC7 is a VDR antagonist, which can be synthesized from 7-dehydrocholesterol (6) in two steps, inhibits VDR selectively, suppresses the viability of cancer cell-lines, and reduces the growth of the spontaneous transgen... |
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T68875 |
Xylocydine
|
|
|
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Xylocydine is a novel Cdk inhibitor, which is an effective inducer of apoptosis in hepatocellular carcinoma cells in vitro and in vivo. Xylocydine also strongly inhibits the activity of Cdk7 and Cdk9, in vitro as well as... |
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T69589 |
PX-316
|
|
|
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PX-316 is a AKT inhibior. PX-316, when administered intraperitoneally to mice at 150 mg/kg, inhibits Akt activation in HT-29 human tumor xenografts up to 78% at 10 h with recovery to 34% at 48 h. PX-316 has antitumor act... |
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T69922 |
EPZ020411 HCl
|
|
|
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EPZ020411 is a potent and selective PRMT6 inhibitor tool compound. EPZ020411 shows good bioavailability following subcutaneous dosing in rats making it a suitable tool for in vivo studies. EPZ020411 suppresses RCC1 argin... |
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T28271 |
OSI-296
|
|
|
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OSI-296 is a potent and dual inhibitor of cMET and RON kinases (IC50 value are 42 nM and 200 nM for cMet and sfRon respectively) . OSI-206 shows in vivo efficacy and is well tolerated in tumor xenografts models upon oral... |
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T9665 |
Esuberaprost Sodium
|
|
|
|
Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demo... |
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T36192 |
CAY10682
|
|
|
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(±)-Nutlin-3 blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo. CAY10682 is a pyrrolo[3,4c]p... |
|
T71624 |
GB1874
|
|
|
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GB1874 inhibitor of the Wnt pathway that targets the β-cat-TCF4 PPI. GB1874 also affected the proliferation and stemness of Wnt-addicted colorectal cancer (CRC) cells in vitro. Encouragingly, GB1874 inhibited the growth... |
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T62877 |
RET-IN-7
|
|
|
|
RET-IN-7 exhibits strong inhibitory effects against RET kinase in vitro and shows significant efficacy in treating RET-driven tumor xenografts in mice through multiple-day dosing. |
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T28216 |
NTRC 0066-0
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NTRC-0066-0,NTRC-00660,NTRC00660,NTRC0066-0 |
|
|
NTRC-0066-0 is a a highly potent and selective inhibitor of TTK. NTRC 0066-0 inhibits the phosphorylation of a TTK substrate and induces chromosome missegregation. NTRC 0066-0 inhibits tumor growth in MDA-MB-231 xenograf... |
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T39553 |
TAK-960 monohydrochloride
|
|
|
|
TAK-960 monohydrochloride is an orally available compound that selectively inhibits polo-like kinase 1 (PLK1) with an IC 50 of 0.8 nM. It also demonstrates inhibitory activity against PLK2 (IC 50 of 16.9 nM) and PLK3 (IC... |
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T71426 |
STA-1474
|
|
|
|
STA-1474 is a water soluble prodrug of ganetespib (formerly STA-9090). STA-1474 will metabolized to Ganetespib, which is a potent HSP90 inhibitor previously shown to kill canine tumor cell lines in vitro and inhibit tumo... |
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T76558 |
Onvitrelin ucalontide
|
|
|
|
Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is a luteinizing hormone-releasing hormone (LHRH) analogue possessing antineoplastic properties, characterized by the peptide sequence KFAKFAKKFAKFAKKFAKQHWSYGLRPG. It demon... |
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T27866 |
LXY6090
|
LXY 6090,LXY-6090 |
|
|
LXY6090 is a HIF-1 inhibitor. LXY6090 inhibited the activity of HIF-1 and downregulated the protein level of HIF-1α in breast cancer cells. LXY6090 showed in vivo anticancer efficacy by decreasing the HIF-1α expression i... |
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T70345 |
JAS239
|
|
|
|
JAS239 is a novel carbocyanine dye that binds and competitively inhibits choline kinase (ChoK) intracellularly. JAS239 attenuated choline phosphorylation and viability in a panel of human breast cancer cell lines. Antibo... |
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T36458 |
CAY10701
|
CAY10701 |
|
|
CAY10701 is a 7-deazahypoxanthine analog that prevents microtubule formation, blocking the proliferation of HeLa and MCF-7 cells (GI50s = 22 and 38 nM, respectively). It also inhibits the growth of several different colo... |
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T76940 |
Cantuzumab ravtansine
|
|
|
|
Cantuzumab ravtansine (IMGN242; huC242-DM4), an antibody-drug conjugate (ADC), consists of the humanized monoclonal antibody huC242 covalently bonded through a disulfide linkage to the cytotoxic agent DM4 (DM4). This com... |
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T76506 |
Coibamide A
|
|
|
|
Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, exhibits potent antiproliferative activity alongside inducing autophagosome accumulation through an mTOR-independent mechanism and triggering apoptosis. Additio... |
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T36191 |
CAY10681
|
|
|
|
Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-κB signaling. It potently binds MDM2 (Ki = 250 nM)... |
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T68861 |
MS-0022
|
|
|
|
MS-0022 is a SMO antagonist. MS-0022 showed effective Hh signaling pathway inhibition at the level of SMO in the low nM range, and Hh pathway inhibition downstream of Suppressor of fused (SUFU) in the low µM range. MS-00... |
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T64204 |
NU5455
|
|
|
|
NU5455 is a selective, potent, orally active inhibitor of DNA-PKcs. NU5455 enhances the efficacy of locally released doxorubicin in liver tumour xenografts without causing any adverse effects. nU5455 enhances the efficac... |
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T64216 |
TAK-960 hydrochloride
|
|
|
|
TAK-960 hydrochloride is a potent, selective, orally active inhibitor of polo-like kinase 1 (PLK1) (IC50: 0.8 nM). TAK-960 hydrochloride inhibits the proliferation of a variety of tumour cell lines and significantly trea... |
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T60661 |
CP681301
|
|
|
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CP681301 is a potent inhibitor of CDK5 with antiproliferative activity. CP681301 exhibits anti-tumor activity in Drosophila. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in Glioma st... |
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T68324 |
KCN1
|
|
|
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KCN1, a novel synthetic sulfonamide, is a HIF pathway inhibitor with potential anticancer activity in vitro and in vivo anti-pancreatic cancer activities and preclinical pharmacology. KCN1 specifically inhibited HIF repo... |
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T76939 |
Cantuzumab mertansine
|
|
|
|
Cantuzumab mertansine (SB-408075; huC242-DM1), an antibody-drug conjugate (ADC), comprises the potent maytansine derivative (DM1) linked to the humanized monoclonal antibody (huC242) targeting CanAg. Demonstrating cytoto... |
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T71111 |
Famitinib malate
|
SHR1020 malate |
|
|
Famitinib malate (SHR1020) is an orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. It induces... |
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T29172 |
YD277
|
YD 277,YD-277 |
|
|
YD277 is a small molecule derived from ML264, a KLF5 inhibitor that elicits cytotoxic effects in colon cancer cell lines. YD277 significantly induced G1 cell cycle arrest and apoptosis in MDA-MB-231 and MDA-MB-468 TNBC c... |
