m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT03046
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[1] | |||
m6A modification
SETD2
SETD2
METTL16
Methylation
: m6A sites
Direct
Inhibition
Histone modification
H3K36me3
SETD2
UBXN1
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| m6A Modification: | |||||
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| m6A Regulator | Methyltransferase-like 16 (METTL16) | WRITER | |||
| m6A Target | Histone-lysine N-methyltransferase SETD2 (SETD2) | ||||
| Epigenetic Regulation that have Cross-talk with This m6A Modification: | |||||
| Epigenetic Regulation Type | Histone modification (HistMod) | ||||
| Epigenetic Regulator | Histone-lysine N-methyltransferase SETD2 (SETD2) | WRITER | View Details | ||
| Regulated Target | Histone H3 lysine 36 trimethylation (H3K36me3) | View Details | |||
| Downstream Gene | UBXN1 | View Details | |||
| Crosstalk Relationship | m6A → Histone modification | Inhibition | |||
| Crosstalk Mechanism | m6A modification impacts directly histone modification through modulating the expression level of histone-associated enzymes | ||||
| Crosstalk Summary | Furthermore, through the MeRIP-qPCR and dual-luciferase reporter assays, we found that knocking down METTL16 reduced the m6A modification level of the UBXN1 coding sequence in GC. Interestingly, the silencing of METTL16 upregulated the expression of the major Histone H3 lysine 36 trimethylation (H3K36me3) methyltransferase Histone-lysine N-methyltransferase SETD2 (SETD2) in GC cells by methylating the m6A site in the mRNA coding sequence of SETD2 and also downregulated UBXN1 expression by promoting H3K36me3 modification at the UBXN1 promoter. | ||||
| Responsed Disease | Gastric cancer | ICD-11: 2B72 | |||
In-vitro Model |
AGS | Gastric adenocarcinoma | Homo sapiens | CVCL_0139 | |
| MKN28 | Gastric tubular adenocarcinoma | Homo sapiens | CVCL_1416 | ||
| GES-1 | Normal | Homo sapiens | CVCL_EQ22 | ||
| In-vivo Model | AGS cells (1 × 107) transfected with the specified material were combined with 50% (v/v) Matrigel (Corning, MA, USA) and subsequently subcutaneously injected into both the left and right dorsal areas of female BALBc nude mice (SPF, Beijing, China). The AGS cells (1 × 107) was subcutaneously injected weekly. | ||||
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
| 2B72: Gastric cancer | 81 Compound(s) Regulating the Disease | Click to Show/Hide the Full List | ||
| Leniolisib | Approved | [2] | ||
| Synonyms |
1354690-24-6; Leniolisib free base; UNII-L22772Z9CP; (S)-1-(3-((6-(6-methoxy-5-(trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)propan-1-one; L22772Z9CP; 1354690-24-6 (free base); leniolisib(CDZ 173); CDZ173; CDZ-173; 1-[(3S)-3-[[6-[6-methoxy-5-(trifluoromethyl)pyridin-3-yl]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]amino]pyrrolidin-1-yl]propan-1-one; Leniolisib [INN]; Leniolisib (CDZ173); Leniolisib (USAN/INN); CDZ173-NX; SCHEMBL323054; GTPL9424; CHEMBL3643413; BDBM118299; EX-A2854; MFCD30470232; s8752; ZB1510; CS-7524; DC22326; SB18839; Example 67 [WO2012004299]; 1-{(S)-3-[6-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-y; 1-{(S)-3-[6-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-ylamino]-pyrrolidin-1-yl}-propan-1-one; AS-56217; HY-17635; A16796; D11158; US8653092, 67; Q27282602; 1-Propanone, 1-((3S)-3-((5,6,7,8-tetrahydro-6-(6-methoxy-5-(trifluoromethyl)-3-pyridinyl)pyrido(4,3-d)pyrimidin-4-yl)amino)-1-pyrrolidinyl)-; 9NQ
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| Atezolizumab | Approved | [3] | ||
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| Bavencio | Approved | [3] | ||
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| Tebentafusp | Approved | [4] | ||
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| Merimepodib | Approved | [5] | ||
| Synonyms |
Merimebodib; Merimepodib [USAN:INN]; Tyverb/Tykerb; MMPD; 198821-22-6; 2ZL2BA06FU; C23H24N4O6; CHEMBL304087; MERIMEPODIB, VI-21497, VX-497; UNII-2ZL2BA06FU; VI-21497; VX-497; VX497; Vx 497; carbamic acid
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| Taxol | Approved | [6] | ||
| Synonyms |
C47H51NO14; weekly paclitaxel; Micellar Paclitaxel; Paclitaxel [USAN:INN:BAN]; SCHEMBL15000506; Benzenepropanoic acid, beta-(benzoylamino)-alpha-hydroxy-, 6,12b-bis(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca(3,4)benz(1,2-b)oxet-9-yl ester, (2aR-(2aalpha,4beta,4abeta,6beta,9alpha(alphaR*,betaS*),11alpha,12alpha,12aalpha,12balpha))-
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| Ramucirumab | Approved | [7] | ||
| Synonyms |
LY3009806
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| Tucatinib | Approved | [8] | ||
| Synonyms |
Irbinitinib; 937263-43-9; ONT-380; UNII-234248D0HH; 234248D0HH; N6-(4,4-Dimethyl-4,5-dihydrooxazol-2-yl)-N4-(3-methyl-4-((1,2,4)triazolo(1,5-a)pyridin-7-yloxy)phenyl)quinazoline-4,6-diamine; 4,6-Quinazolinediamine, N6-(4,5-dihydro-4,4-dimethyl-2-oxazolyl)-N4-(3-methyl-4-((1,2,4)triazolo(1,5-a)pyridin-7-yloxy)phenyl)-; ONT 380; 4,6-QuinazolinediaMine, N6-(4,5-dihydro-4,4-diMethyl-2-oxazolyl)-N4-[3-Methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-; Tucatinib [USAN:INN]; 6-DIAMINE
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| Antacids | Approved | [9] | ||
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| Trastuzumab | Approved | [3] | ||
| Synonyms |
Herceptin; Herceptin (TN); Trastuzumab (INN); Trastuzumab (genetical recombination); Trastuzumab (genetical recombination) (JAN); Trastuzumab (ERBB2 mAb inhibitor)
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| Carbamazepine | Phase 3 | [10] | ||
| Synonyms |
Carbamazepine (iv, epilepsy); Carbamazepine (iv, epilepsy), Lundbeck; Carbamazepine (iv, epilepsy), Ovation Pharmaceuticals
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| Margetuximab | Approved | [3] | ||
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| Nivolumab | Approved | [3] | ||
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| GRANITE | Phase 3 | [11] | ||
| Synonyms |
Penoxsulam; 219714-96-2; 2-(2,2-difluoroethoxy)-N-(5,8-dimethoxy-[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide; UNII-784ELC1SCZ; 784ELC1SCZ; CHEBI:81776; 2-(2,2-difluoroethoxy)-n-(5,8-dimethoxy[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide; Penoxsulam [ISO]; PXD; DSSTox_CID_14803; DSSTox_RID_79204; DSSTox_GSID_34803; SCHEMBL116968; CHEMBL1895913; DTXSID0034803; HSDB 7887; AMY12535; BCP18718; EBD18529; Tox21_301010; MFCD07363876; ZINC13827750; AKOS025401685; NCGC00163715-01; NCGC00163715-02; NCGC00163715-03; NCGC00254912-01; AC-24494; Penoxsulam 100 microg/mL in Acetonitrile; CAS-219714-96-2; FT-0696708; Penoxsulam, PESTANAL(R), analytical standard; C18481; Q22808507; 2-(2,2-Difluoroethoxy)-6-trifluoromethyl-N-(5, 8-dimethoxy[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)benzenesulfonamide; 2-(2,2-Difluoroethoxy)-N-(5,8-dimethoxy[1,2,4]-triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide; 2-(2,2-difluoroethoxy)-N-{5,8-dimethoxy-[1,2,4]triazolo[1,5-c]pyrimidin-2-yl}-6-(trifluoromethyl)benzene-1-sulfonamide; 2-(2,2-difluoroethyl)-N-(5,8-dimethoxy[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide; Benzenesulfonamide, 2-(2,2-difluoroethoxy)-N-(5,8-dimethoxy(1,2,4)triazolo(1,5-c)pyrimidin-2-yl)-6-(trifluoromethyl)-
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| Zolbetuximab | Phase 3 | [12] | ||
| Synonyms |
IMAB362
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| Tusamitamab ravtansine | Phase 3 | [13] | ||
| Synonyms |
SAR408701
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| Andecaliximab | Phase 3 | [14] | ||
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| ABP 980 | Phase 3 | [15] | ||
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| GS-5745 | Phase 3 | [6] | ||
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| S-1 | Phase 3 | [16] | ||
| Synonyms |
Ciprofibrate-coa; Ciprofibrate-coenzyme A; Coenzyme A, ciprofibrate-; AC1L4TRG; AC1Q3T4H; 111900-25-5; s-{1-[(2r,3s,4r,5r)-5-(6-amino-9h-purin-9-yl)-4-hydroxy-3-(phosphonooxy)tetrahydrofuran-2-yl]-3,5,9-trihydroxy-8,8-dimethyl-3,5-dioxido-10,14-dioxo-2,4,6-trioxa-11,15-diaza-3; E5,5; E5-diphosphaheptadecan-17-yl} 2-[4-(2,2-dichlorocyclopropyl)phenoxy]-2-methylpropanethioate(non-preferred name); Coenzyme A, S-(2-(4-(2,2-dichlorocyclopropyl)phenoxy)-2-methylpropanoate)
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| Lonsurf | Phase 3 | [3] | ||
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| GDC-0068 | Phase 3 | [6] | ||
| Synonyms |
RG7440
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| Edotecarin | Phase 3 | [17] | ||
| Synonyms |
ED-749; Edotecarin < Prop INN; J-107088; PF-804950; 12-(beta-D-Glucopyranosyl)-2,10-dihydroxy-6-[2-hydroxy-1-(hydroxymethyl)ethylamino]-6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-dione
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| RG3638 | Phase 3 | [18] | ||
| Synonyms |
Onartuzumab
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| G17DT | Phase 3 | [19] | ||
| Synonyms |
Gastrimmune; Insegia
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| DE-766 | Phase 3 | [20] | ||
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| Tesetaxel | Phase 2 | [21] | ||
| Synonyms |
DJ-927; 333754-36-2; UNII-UG97LO5M8Y; UG97LO5M8Y; Tesetaxel [INN]; DJ927; DJ 927; CHEMBL2107787; SCHEMBL12060837; DB12019; Z-3104; (2AS,2BR,3S,4S,6S,8AR,10R,11AS,11BR,13AR)-2A-ACETOXY-6-(((2R,3S)-3-((TERT-BUTOXYCARBONYL)AMINO)-3-(3-FLUOROPYRIDIN-2-YL)-2-HYDROXYPROPANOYL)OXY)-10-((DIMETHYLAMINO)METHYL)-4-HYDROXY-7,11B,14,14-TETRAMETHYL-2A,2B,3,4,5,6,8A,11A,11B,12,13,13A-DODECAHYDRO-2H-4,8-METHANOOXETO[3'',2'':3',4']BENZO[1',2':3,4]CYCLODECA[1,2-D][1,3]DIOXOL-3-YL BENZOATE
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| Nelipepimut S | Phase 3 | [22] | ||
| Synonyms |
E75
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| BMS-986205 | Phase 3 | [3] | ||
| Synonyms |
KRTIYQIPSAGSBP-KLAILNCOSA-N; 1923833-60-6; BMS986205; UNII-0A7729F42K; 0A7729F42K; GTPL9707; SCHEMBL18826792; SCHEMBL17740982; SCHEMBL19105151; EX-A2606; AKOS032954040; HY-101560; CS-0021719; Q29213697; (R)-N-(4-chlorophenyl)-2-((1s,4S)-4-(6-fluoroquinolin-4-yl)cyclohexyl)propanamide; (2R)-N-(4-chlorophenyl)-2-[4-(6-fluoroquinolin-4-yl)cyclohexyl]propanamide; (2R)-N-(4-Chlorophenyl)-2-(4-(6-fluoro-4-quinolyl)cyclohexyl)propanamide, cis; Cyclohexaneacetamide, N-(4-chlorophenyl)-4-(6-fluoro-4-quinolinyl)-alpha-methyl-, cis-(alphaR)-
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| Rivoceranib | Phase 3 | [3] | ||
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| Claudiximab | Phase 3 | [3] | ||
| Synonyms |
IMAB-362; Anti-GC182 mAbs (cancer), Ganymed; Anti-GC182 monoclonal antibodies (cancer), Ganymed; Anti-CLDN18-2 mAbs (cancer), Ganymed; Anti-CLDN18-2 monoclonal antibodies (cancer), Ganymed
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| OS-440 | Phase 3 | [23] | ||
| Synonyms |
CNS modulator (spasticity), Osmotica
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| Oraxol | Phase 3 | [3] | ||
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| ICI 118,551 | Phase 3 | [6] | ||
| Synonyms |
Ici 118551; (2R,3S)-1-[(7-methyl-2,3-dihydro-1H-inden-4-yl)oxy]-3-(propan-2-ylamino)butan-2-ol; CHEMBL198059; CHEBI:73289; ICI-118551; ICI118551; erythro-DL-1-(7-Methylindan-4-yloxy)-3-isopropylaminobutan-2-ol; (2R,3S)-3-(isopropylamino)-1-[(7-methyl-2,3-dihydro-1H-inden-4-yl)oxy]butan-2-ol; 2-Butanol, 1-((2,3-dihydro-7-methyl-1H-inden-4-yl)oxy)-3-((1-methylethyl)amino)-, (2R,3S)-rel-; 2-Butanol, 1-((2,3-dihydro-7-methyl-1H-inden-4-yl)oxy)-3-((1-methylethyl)amino)-, (R*,S*)-(+-)-; ICI-118,551; Ici 111,581; AC1NUNSO
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| Evorpacept | Phase 2/3 | [24] | ||
| Synonyms |
ALX148
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| BNT141 | Phase 2 | [25] | ||
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| Anti-LAG3 | Phase 2 | [15] | ||
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| GSK1292263 | Phase 2 | [26] | ||
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| MM-111 | Phase 2 | [27] | ||
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| Plevitrexed | Phase 2 | [28] | ||
| Synonyms |
ZD 9331; ZD9331; 153537-73-6; Plevitrexed [INN]; ZD-9331; NSC 696259; UNII-L9P2881C3H; CHEMBL126648; (2s)-2-[(2-fluoro-4-{[(4-hydroxy-2,7-dimethylquinazolin-6-yl)methyl](prop-2-yn-1-yl)amino}benzoyl)amino]-4-(2h-tetrazol-5-yl)butanoic acid; L9P2881C3H; Plevitrexed (INN); 172521-94-7; (2S)-2-[[4-[(2,7-dimethyl-4-oxo-1H-quinazolin-6-yl)methyl-prop-2-ynylamino]-2-fluorobenzoyl]amino]-4-(2H-tetrazol-5-yl)butanoic acid; 1H-Tetrazole-5-butanoic acid,
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| DS-8201 | Phase 1 | [15] | ||
| Synonyms |
9-Aminofluorene; 9H-Fluoren-9-amine; 525-03-1; FLUOREN-9-AMINE; Fluoren-9-ylamine; UNII-4NHO2K4K5B; CCRIS 7000; BRN 2209545; 4NHO2K4K5B; OUGMRQJTULXVDC-UHFFFAOYSA-N; fluorene-9-ylamine; 9-Amino-fluoren; 9-amino-fluorene; 9H-9-fluorenamine; 9H-fluoren-9-yl-amine; AC1L1VP5; 4-12-00-03390 (Beilstein Handbook Reference); SCHEMBL353865; AC1Q53A2; AC1Q53A1; KS-00000JGC; CTK1H0380; DTXSID90200496; MolPort-001-794-448; HMS1780P20; 9H-fluoren-9-ylamine hydrochloride; ZINC1724407; ALBB-023296; CA-733; SBB005783; AKOS000264388; MCULE-8757055914; DS-
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| XL880 | Phase 2 | [29] | ||
| Synonyms |
GSK 089; GSK 1363089; GSK1363089; XL 880; GSK1363089, GSK089, foretinib, EXEL-2880, XL880; 88Z; MET inhibitors
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| Matuzumab | Phase 2 | [30] | ||
| Synonyms |
EMD-62000; EMD-72000; Anti-EGF receptor humanized antibody (iv, cancer), Merck KGaA/ Takeda Pharmaceuticals; Anti-EGFR humanized mAb (iv, cancer), Merck KGaA/ Takeda Pharmaceuticals; Anti-epidermal growth factor receptor humanized antibody (iv, cancer), Merck KGaA/ Takeda Pharmaceuticals
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| BAY-57-9352 | Phase 2 | [6] | ||
| Synonyms |
Telatinib; Bay 57-9352
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| Bemarituzumab | Phase 2 | [31] | ||
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| PEGPH20 | Phase 2 | [3] | ||
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| Plevitrexed (R)-isomer | Phase 2 | [32] | ||
| Synonyms |
YW3548
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| APR-246 | Phase 2 | [33] | ||
| Synonyms |
Eprenetapopt
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| CRS-207 | Phase 2 | [22] | ||
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| Opdivo + Yervoy | Phase 3 | [3] | ||
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| CT-041 | Phase 1/2 | [34] | ||
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| BPX-601 | Phase 1/2 | [35] | ||
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| Anti-MUC1 CAR-T cells | Phase 1/2 | [36] | ||
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| Anti-Mesothelin CAR-T cells | Phase 1/2 | [37] | ||
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| Anti-HER2 CAR-T | Phase 1/2 | [38] | ||
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| CAR-T Cells targeting EpCAM | Phase 1/2 | [39] | ||
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| PAT-SC1 | Phase 1/2 | [40] | ||
| Synonyms |
SC-1; Adjuvant therapy (gastric cancer), University of Wurzburg; SC-1 (gastric cancer), CAT; SC-1 (gastric cancer), Debiopharm; SC-1 (gastric cancer), Patrys; SC-1 (stomach cancer), OncoMab
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| ASP2138 | Phase 1 | [41] | ||
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| SAR443216 | Phase 1 | [42] | ||
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| AMG 199 | Phase 1 | [43] | ||
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| AMG 910 | Phase 1 | [44] | ||
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| Alofanib | Phase 1 | [45] | ||
| Synonyms |
1612888-66-0; 3-(N-(4-methyl-2-nitro-5-(pyridin-3-yl)phenyl)sulfamoyl)benzoic acid; RPT-835(alofanib); UNII-LQX7RFK8MZ; RPT-835; RPT835; LQX7RFK8MZ; ES000835; Alofanib [INN]; Alofanib(RPT835); Syn007154; CHEMBL4594436; SCHEMBL18660613; AMY16650; BCP31905; EX-A2731; MFCD30533418; NSC790182; s8754; Benzoic acid, 3-(((4-methyl-2-nitro-5-(3-pyridinyl)phenyl)amino)sulfonyl)-; NSC-790182; SB19665; AC-31695; AK668992; AS-56846; HY-17601; CS-0014684; RPT 835; Q27283135; 3-{[4-methyl-2-nitro-5-(pyridin-3-yl)phenyl]sulfamoyl}benzoic acid
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| HER2-specific CAR T cell | Phase 1 | [46] | ||
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| Anti-CEA-CAR T | Phase 1 | [47] | ||
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| XR-5944 | Phase 1 | [48] | ||
| Synonyms |
MLN-944; XR-11576 analogs; XR-5000 analogs; XR-5942
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| A168 | Phase 1 | [49] | ||
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| EGFR806-specific CAR T cell | Phase 1 | [50] | ||
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| AbGn-107 | Phase 1 | [3] | ||
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| FPA144 | Phase 1 | [15] | ||
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| Minnelide 001 | Phase 1 | [6] | ||
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| CAR-T cells targeting EpCAM | Phase 1 | [51] | ||
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| Anti-CEA CAR-T cells | Phase 1 | [52] | ||
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| EPCAM-targeted CAR-T cells | Clinical trial | [53] | ||
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| PMID28460551-Compound-1 | Patented | [54] | ||
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| Conjugated 3-(indolyl)-and 3-(azaindolyl)-4-arylmaleimide compound 1 | Patented | [55] | ||
| Synonyms |
PMID28621580-Compound-WO2012084683c62
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| TOPIXANTRONE HYDROCHLORIDE | Discontinued in Phase 2 | [56] | ||
| Synonyms |
SCHEMBL1418986; Topixantrone hydrochloride < Prop INNM; BBR-3409 (dimaleate); 5-[2-(Dimethylamino)ethylamino]-2-[2-(2-hydroxyethylamino)ethyl]indazolo[4,3-gh]isoquinolin-6(2H)-one dihydrochloride
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| MDL 101,731 | Discontinued in Phase 2 | [57] | ||
| Synonyms |
Tezacitabine; Fmdc cpd; 130306-02-4; UNII-7607Y95N9S; Mdl 101731; (E)-2'-Deoxy-2'-(fluoromethylene) cytidine; MDL-101731; 2'-Deoxy-2'-(fluoromethylene)cytidine; 7607Y95N9S; Cytidine, 2'-deoxy-2'-(fluoromethylene)-, (2E)-; (E)-2'-Deoxy-2'-(fluoromethylene)cytidine; Tezacitabine [INN]; tezaciabine; Tezacitabine, anhydrous; AC1O5KIG; SCHEMBL18724; SCHEMBL18725; Tezacitabine, anhydrous [INN]; CHEMBL2105467; C10H12FN3O4; DTXSID10156446; GFFXZLZWLOBBLO-ASKVSEFXSA-N; ZINC3777826; KW-2331
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| BBR-3438 | Discontinued in Phase 2 | [58] | ||
| Synonyms |
Nortopixantrone; UNII-PH2639TAB4; PH2639TAB4; Nortopixantrone [INN:BAN]; AC1MI4ZO; CHEMBL150303; SCHEMBL7804438
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| IPI-493 | Discontinued in Phase 1 | [59] | ||
| Synonyms |
[(3R,5R,6S,7R,8E,10R,11R,12Z,14E)-21-amino-6-hydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16,20,22-trioxo-17-azabicyclo[16.3.1]docosa-1(21),8,12,14,18-pentaen-10-yl] carbamate; AC1NS08X; SCHEMBL16226496; SCHEMBL16225851
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| Kanjinti | Application submitted | [3] | ||
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| Anti-CD9 mab | Investigative | [60] | ||
| Synonyms |
ALB-6; Anti-CD9 mAb (gastric cancer); Anti-CD9 mAb (gastric cancer), Osaka University
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References
: m6A sites