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T8684 |
Sotorasib
|
AMG-510 |
Ras
|
|
Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib ... |
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T60021 |
EcMetAP-IN-1
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Others
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ecMetAP-IN-1 can be used as a QSAR model to study methionine aminopeptidase inhibitor as an anticancer agent using multiple linear regression. |
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T10252L2 |
ADU-S100 ammonium salt
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ML RR-S2 CDA ammonium salt,MIW815 ammonium salt |
STING
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T39584 |
MI-3454
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|
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MI-3454 is a highly potent, orally active, and selective inhibitor of the interaction between menin and MLL1, with an IC50 of 0.51 nM. This compound effectively inhibits the proliferation of leukemic cells and promotes t... |
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T15249 |
Estrogen receptor modulator 1
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Estrogen Receptor/ERR
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Estrogen receptor modulator 1 causes regression of Tamoxifen-resistant, hormone-independent xenograft tumors. Estrogen receptor modulator 1 is an orally active and selective estrogen receptor modulator (SERM) (pIC50: 0.4... |
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T70388 |
(S)-Enitociclib
|
VIP152 |
CDK
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|
(S)-Enitociclib (VIP152) is a selective CDK9 inhibitor that induces complete regression of MYC+ lymphomas by inhibiting RNA polymerase II-mediated transcription of anti-apoptotic and pro-survival proteins. |
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T78211 |
STX-478
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PI3K
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STX-478 (compound 80), an orally administered, CNS-penetrant allosteric mutant-selective PI3Kα inhibitor, demonstrates significant and sustained tumor regression, making it a valuable agent in cancer research [1]. |
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T9429 |
ZZW-115
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|
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ZZW-115 is a potent NUPR1 inhibitor with a Kd of 2.1 μM. ZZW-115 is a derivative of Trifluoperazine (TFP). ZZW-115 shows a dose-dependent tumor regression with no neurological side effects and induces cell death mainly b... |
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T36287 |
Pirtobrutinib
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BTK
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|
Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to t... |
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T18680 |
SD-36
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Others
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SD-36, a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), exhibits high specificity for STAT3 over other STAT members. It effectively targets both wild-type and mutated STAT3 proteins in cells, inhibiting their ... |
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T2576 |
Brivanib (alaninate)
|
BMS-582664,Brivanib Alaninate |
VEGFR
,
FGFR
,
Autophagy
|
|
Brivanib Alaninate (BMS-582664) is the alaninate salt of a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic activity. Brivanib strongly binds to and inhibits VEGFR2, a tyrosi... |
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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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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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T35273 |
YPC-22026
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YPC22026,YPC 22026 |
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YPC-22026 is a novel tumor regression inducer that inhibits the znf143 regulatory gene in the mouse xenotransplantation model. |
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T69479 |
CGC 11093
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|
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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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T22290 |
CFT-743
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Others
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CFT-0743 could inhibits tumor growth (81% regression) potently with PDC50 value of 0.18 nM. |
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T38050 |
CP-609754
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Transferase
|
|
CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 n... |
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T39938 |
M-1211
|
|
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M 1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression. |
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T41205 |
3',3'-cGAMP sodium salt
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3',3'-cGAMP sodium salt is a STING agonist. Reduces B cell proliferation and induces apoptosis of malignant B cellsin vitro. Suppresses 5TGM1 multiple myeloma xenograft growth in immunodeficient mice, and induces leukemi... |
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T40223 |
EEDi-5273
|
|
|
|
EEDi-5273 is a highly potent and orally efficacious inhibitor of EED, with an approximate IC50 value of 0.2 nM. This compound exhibits exceptional activity, capable of achieving complete and persistent regression of tumo... |
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T11396 |
GGTI-2418
|
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Transferase
|
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GGTI-2418 is a highly potent, competitive, and selective inhibitor of geranylgeranyltransferase I (GGTase I), showing inhibitory activities with IC50 values of 9.5 nM for GGTase I and 53 μM for FTase, respectively. Addit... |
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T70356 |
F-1394
|
|
|
|
F-1394 is an acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. F-1394 both prevents the formation of atherosclerosis and accelerates its regression without affecting the serum TC level, indicating that F-1394 acts ... |
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T79461 |
YK-029A
|
|
EGFR
|
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YK-029A, an orally active EGFR mutant inhibitor, targets both EGFR T790M and EGFRex20ins mutations. It demonstrates notable antitumor efficacy, inducing tumor regression in EGFRex20ins-driven patient-derived xenograft (P... |
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T74975 |
Zn-DPA-maytansinoid conjugate 1
|
|
|
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Zn-DPA-maytansinoid conjugate 1, a small molecule-based immune checkpoint-targeting maytansinoid conjugate, effectively induces sustained tumor growth regression and transforms the tumor microenvironment (TME) into an "i... |
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T78442 |
TSPP tetrasodium
|
|
|
|
TSPP tetrasodium, a photosensitizer, has demonstrated significant efficacy in the in vivo regression of cancer and microbial infections (Ex: 413 nm, Em: 640 nm) [1][2]. |
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T63328 |
AMXI-5001 hydrochloride
|
|
|
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AMXI-5001 hydrochloride is an orally active and potent inhibitor of parp1/2 and microtubule polymerization with significantly lower IC50 values than existing clinical PARP1/2 inhibitors. mxi-5001 hydrochloride exhibits s... |
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T71023 |
MI-888 free base
|
|
|
|
MI-888 is a potent MDM2 inhibitor (Ki = 0.44 nM) with a superior pharmacokinetic profile and enhanced in vivo efficacy. MI-888 is capable of achieving rapid, complete, and durable tumor regression in two types of xenogra... |
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T32026 |
GYKI-13324
|
GYKI 13324,GYKI13324 |
|
|
GYKI-13324 is bifunctional nitrosoureido derivative and alkylating agent. GYKI-13324 was studied on human colorectal tumor xenograft lines. Given orally in single or multiple daily doses, GYKI-13324 produced long-term or... |
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T36201 |
AZD5582 dihydrochloride
|
AZD 5582 dihydrochloride |
|
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Dimeric Smac mimetic; potent inhibitor of X-linked (XIAP) and cellular (cIAP) inhibitor of apoptosis protein (IC50 values are 15, 15 and 21 nM for XIAP, cIAP1 and cIAP2 respectively). Binds to the BIR3 domain of XIAP to ... |
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T77115 |
Plamotamab
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|
|
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Plamotamab (XmAb-13676), a human bispecific antibody (bsAb) targeting CD3 and CD20, recruits cytotoxic T cells to eliminate CD20-expressing tumor cells. It demonstrates mild hematologic reaction (MR) and effectively indu... |
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T64015 |
FGFR4-IN-6
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|
|
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FGFR4-IN-6 is a covalent, reversible FGFR4 inhibitor (IC50: 5.4 nM) that exhibits good oral pharmacokinetic properties. In a xenograft mouse model of the Hep3B2.1-7 HCC cell line, FGFR4-IN-6 was able to significantly ind... |
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T74749 |
AK-2292
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|
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AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC 50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and c... |
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T70588 |
Tazemetostat HCl
|
|
|
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Tazemetostat HCl is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. EPZ-6438 induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells. Treatment of... |
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T9684 |
(Z)-Orantinib
|
|
|
|
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC 50 s of 2.1, 0.008, and 1.2 μM, respectively. (Z)-Orantinib is a potent antiangiogen... |
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T34278 |
Redaporfin
|
F 2BMet,F2BMet,F-2BMet,LUZ11,LUZ 11,LUZ-11 |
|
|
Redaporfin, also known as F-2BMet or LUZ-11, is a photosensitizer for Photodynamic Therapy (PDT) of cancer. Redaporfin showed a high efficacy in the treatment of male BALB/c mice with subcutaneously implanted colon (CT26... |
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T78804 |
PI3Kα-IN-12
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|
PI3K
|
|
PI3Kα-IN-12 (compound 13), a potent and selective PI3Kα inhibitor (IC50: 1.2 nM), effectively suppresses HCT-116 and U87-MG cell proliferation with IC50 values of 0.83 and 1.25 μM, respectively. Intraperitoneal administr... |
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T70552 |
Ipatasertib tosylate
|
|
|
|
Ipatasertib, also known as GDC0068, is an orally active, potent and selective Akt inhibitor. GDC-0068 blocked Akt signaling both in cultured human cancer cell lines and in tumor xenograft models. Inhibition of Akt acti... |
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T78836 |
IHMT-PI3K-455
|
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PI3K
|
|
IHMT-PI3K-455 (Compound 15u) is a potent, selective PI3Kγ/δ dual inhibitor, demonstrating oral activity, with IC50 values of 7.1 nM for PI3Kγ and 0.57 nM for PI3Kδ. This compound inhibits AKT phosphorylation and promotes... |
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T36404 |
PRLX-93936
|
|
|
|
PRLX-93936 is an analog of erastin that has antitumor activity. It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay). PRLX-93936 (1... |
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T80750 |
YN14
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|
PROTACs
|
|
YN14 is a highly potent and selective KRASG12C proteolysis targeting chimera (PROTAC) capable of forming a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). It exhibits antiproliferative effec... |
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T62847 |
AMXI-5001
|
|
|
|
AMXI-5001 is a potent, orally active inhibitor of parp1/2 and microtubule aggregation. mxi-5001 shows selective anti-tumour cytotoxicity against a wide range of human cancer cells with IC50s well below those of existing ... |
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T36314 |
Wortmannin-Rapamycin Conjugate
|
|
|
|
Phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) act synergistically in promoting cancer. Wortmannin is a potent inhibitor of PI3K enzymes, while rapamycin blocks mTOR Complex 1 TORC1. Wortmannin... |
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T64277 |
ODN 1585
|
|
|
|
ODN 1585 is a potent inducer of IFN and TNFα production, a potent stimulator of NK (natural killer) and can be used as a vaccine adjuvant.ODN 1585 enhances the function of CD8+ T cells, including CD8+ T cell-mediated IFN... |
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T70779 |
BPR1J-340
|
|
|
|
BPR1J-340 is a potent and selective FLT3 inhibitor with potential anticancer activity. BPR1J-340 was identified as a novel potent FLT3 inhibitor by biochemical kinase activity (IC50 approximately 25 nM) and cellular prol... |
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T82517 |
DYSP-C34
|
|
|
|
DYSP-C34, a potent ultrasound (US)-triggered multifunctional molecular machine, exhibits a favorable lipophilic/hydrophilic balance, enhanced US-induced reactive oxygen species (ROS) production, and improved cellular per... |
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TMIH-0124 |
Brivanib Alaninate-d4
|
|
|
|
Brivanib Alaninate-d4 is a deuterated compound of Brivanib Alaninate. Brivanib Alaninate has a CAS number of 649735-63-7. Brivanib Alaninate is the alaninate salt of a vascular endothelial growth factor receptor 2 (VEGFR... |
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T68497 |
FI-700
|
|
|
|
FI-700 is a novel and potent FLT3 inhibitor with promising antileukemia activity. FI-700 showed a potent IC(50) value against FLT3 kinase at 20 nmol/L in an in vitro kinase assay. FI-700 showed selective growth inhibitio... |
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T70222 |
Ethonafide
|
|
|
|
Ethonafide is an anthracene-containing derivative of amonafide that belongs to the azonafide series of anticancer agents. The lack of cross-resistance in multidrug-resistant cancer cell lines and the absence of a quinone... |
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T68389 |
LY2457546
|
|
|
|
LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 ... |
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T37130 |
MRTX1133 formic
|
|
|
|
MRTX1133 is a highly selective, first-in-class inhibitor of KRAS G12D. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tu... |
