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Zamzetoclax

It’s only fair to share… Zamzetoclax CAS 2388470-64-0 MF C38H46ClN5O6S MW736.32 N-[(3′R,4S,6′R,7′S,8′E,11′S)-7-chloro-7′-methoxy-11′-methyl-13′,15′-dioxospiro[2,3-dihydro-1H-naphthalene-4,22′-20-oxa-13λ6-thia-1,14-diazatetracyclo[14.7.2.03,6.019,24]pentacosa-8,13,16(25),17,19(24)-pentaene]-13′-yl]-3-methoxy-1-methylpyrazole-4-carboxamide B-cell lymphoma 2 (Bcl-2) inhibitor, antineoplastic, RRS8GZU2UN Zamzetoclax (compound 1) is a potential Mcl-1 inhibitor. REFDiscovery of an Oral, Beyond-Rule-of-Five Mcl-1 Protein–Protein Interaction Modulator with the Potential of Treating Hematological Malignancies Publication Name: Journal of Medicinal Chemistry Publication Date: 2023-04-28 PMID: 37114951 DOI: 10.1021/acs.jmedchem.2c01953 SYN WO 2019/222112 https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2019222112&_cid=P12-MJ7Z15-98773-1 Example …

Vilzemetkib

It’s only fair to share… Vilzemetkib CAS 1363402-44-1 MF C36H36F2N4O5 MW 642.7 g/mol 1-N‘-[4-[7-[[1-(cyclopentylamino)cyclopropyl]methoxy]-6-methoxyquinolin-4-yl]oxy-3-fluorophenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide hepatocyte growth factor receptor inhibitor, antineoplastic, AL 2846, FJ4Y6XP24Y Vilzemetkib (also known as AL2846) is an investigational, orally active small-molecule drug that acts as a potent inhibitor of the c-Met receptor tyrosine kinase, a protein often overexpressed in cancers, aiming to block tumor growth, …

Vicadrostat

It’s only fair to share… Vicadrostat CAS 1868065-21-7 MF C15H12ClN3O3 MW 317.73 2-chloro-4-[(6R)-6-(hydroxymethyl)-6-methyl-4-oxo-6,7-dihydropyrano[3,4-d]imidazol-3(4H)-yl]benzonitrilealdosterone synthase inhibitor, BI 690517, AF4VW4GA3H Vicadrostat is an aldosterone synthase inhibitor (IC50=48 nM). Vicadrostat can be used for research in kidney diseases and cardiovascular diseases Vicadrostat (BI 690517) is an investigational drug by Boehringer Ingelheim that selectively blocks aldosterone synthase, reducing excess aldosterone linked to kidney, heart, …

Varegacestat

It’s only fair to share… Varegacestat CAS 1584647-27-7 MF C26H25F7N4O3 MW574.5 (2R,3S)-N1-[(3S)-5-(3-fluorophenyl)-9-methyl-2-oxo-2,3-dihydro-1H1,4-benzodiazepin-3-yl]-2,3-bis(3,3,3-trifluoropropyl)butanediamide (2R,3S)-N1-((3S)-5-(3-FLUOROPHENYL)-2,3-DIHYDRO-9-METHYL-2-OXO-1H-1,4-BENZODIAZEPIN-3-YL)-2,3-BIS(3,3,3-TRIFLUOROPHENYL)BUTANEDIAMIDE(2R,3S)-N1-((3S)-5-(3-FLUOROPHENYL)-9-METHYL-2-OXO-2,3-DIHYDRO-1H-1,4-BENZODIAZEPIN-3-YL)-2,3-BIS(3,3,3-TRIFLUOROPHENYL)BUTANEDIAMIDEgamma-secretase inhibitor, antineoplastic, AL102, BMS 986115, LSK1L593UU, AL 102 BMS-986115 has been used in trials studying the treatment of Various Advanced Cancer. Varegacestat is an orally bioavailable, gamma secretase (GS) and pan-Notch inhibitor, with potential antineoplastic activity. Upon administration, varegacestat binds to GS …

Tigozertinib

It’s only fair to share… Tigozertinib CAS 2660250-10-0 MF C28H37FN6O3S MW 556.7 3-Isoquinolinamine, N-[2-[(3S,4R)-3-fluoro-4-methoxy-1-piperidinyl]-4-pyrimidinyl]-5-(1-methylethyl)-8-[(2R,3S)-2-methyl-3- [(methylsulfonyl)methyl]-1-azetidinyl]- N-{2-[(3S,4R)-3-fluoro-4-methoxypiperidin-1-yl]pyrimidin-4-yl}-8-{(2R,3S)-3-[(methanesulfonyl)methyl]-2-methylazetidin-1-yl}-5-(propan-2-yl)isoquinolin-3-amine N-[2-[(3S,4R)-3-fluoro-4-methoxypiperidin-1-yl]pyrimidin-4-yl]-8-[(2R,3S)-2-methyl-3-(methylsulfonylmethyl)azetidin-1-yl]-5-propan-2-ylisoquinolin-3-amine N-(2-((3S,4R)-3-fluoro-4-methoxypiperidin-l-yl)pyrimidin-4-yl)-5-isopropyl-8-(3-(methylsulfonylmethyl)azetidin-l-yl)isoquinolin-3-amine epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, antineoplastic, PA4PTH5HL9, BLU 945 Tigozertinib (BLU-945) is currently under investigation in clinical trial NCT04862780 (Phase 1/​2 Study Targeting EGFR Resistance Mechanisms in NSCLC) for the treatment of NSCLC. Tigozertinib …

Tambiciclib

It’s only fair to share… Tambiciclib CAS 2247481-08-7 MF C25H35ClN6O2S, 519.10 4-[[[4-[5-chloro-2-[[4-[[(2R)-1-methoxypropan-2-yl]amino]cyclohexyl]amino]-4-pyridinyl]-1,3-thiazol-2-yl]amino]methyl]oxane-4-carbonitrile 2H-PYRAN-4-CARBONITRILE, 4-(((4-(5-CHLORO-2-((TRANS-4-(((1R)-2-METHOXY-1-METHYLETHYL)AMINO)CYCLOHEXYL)AMINO)-4-PYRIDINYL)-2-THIAZOLYL)AMINO)METHYL)TETRAHYDRO- cyclin-dependent kinase inhibitor, antineoplastic, GFH 009, JSH 009, XDZ7VK8CXC, Orphan Drug , Acute myeloid leukaemia, Peripheral T-cell lymphoma Tambiciclib (GFH009, JSH-009) is an orally active, highly potent and selective CDK9 inhibitor (IC50 = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent …

Talorasib

It’s only fair to share… Talorasib CAS 2648584-48-7 MFC32H34ClFN6O3 MW605.10 [(2S)-4-[(7S)-7-(8-chloronaphthalen-1-yl)-2-{[(2S)-1-methylpyrrolidin-2-yl]methoxy}-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-4-yl]-1-(2-fluoroprop-2-enoyl)piperazin-2-yl]acetonitrileKirsten rat sarcoma viral oncogene homologue (KRAS)inhibitor, antineoplastic, 727W6T7DPK SYN CN115385923 https://patentscope.wipo.int/search/en/detail.jsf?docId=CN380619664&_cid=P20-MJ0TAW-52678-1 Preparation Example 1: Synthesis of the compound shown in formula (I)         (1) Synthesis of Compound 1         Synthetic route of compound 1:  Synthesis of compound 1-j         1-Bromo-8-chloronaphthalene (500 mg, 2.07 mmol) was dissolved in …

Talogreptide mesaroxetan

It’s only fair to share… Talogreptide mesaroxetan CAS 1801418-23-4 MF C86H140N22O18 MW1770.17 {MeCOSar}-PEG4-{d-Phe}-Gln-Trp-Ala-Val-Gly-His-{Sta}-Leu-NH2 (2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-[3-[2-[2-[2-[2-[[5-[(8-methyl-3,6,10,13,16,19-hexazabicyclo[6.6.6]icosan-1-yl)amino]-5-oxopentanoyl]amino]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]-3-phenylpropanoyl]amino]pentanediamide N-{21-[(8-methyl-3,6,10,13,16,19-hexaazabicyclo[6.6.6]icosan-1-yl)amino] -17,21-dioxo-4,7,10,13-tetraoxa-16-azahenicosan-1-oyl}-D-phenylalanyl-L-glutaminyl-L-tryptophyl-L-alanyl-Lvalylglycyl-L-histidyl-(3S,4S)-4-amino-3-hydroxy-6-methylheptanoyl-L-leucinamidediagnostic imaging agent, antineoplastic, ZUN64K4H2X, SAR-BBN Talogreptide mesaroxetan (CAS 1801418-23-4) is a synthetic peptide, a complex molecule used as a diagnostic imaging agent with potential antitumor effects, targeting G-protein coupled receptors (GRPr) often overexpressed in cancers, allowing for specific tumor visualization …

Suvadronabinol

It’s only fair to share… Suvadronabinol CAS 1225194-84-2 MF C30H43NO6 MW513.7 g/mol 4-{[(2S)-3-methyl-1-oxo-1-{[(6aR,10aR)-6,6,9-trimethyl-3-pentyl6a,7,8,10a-tetrahydro-6H-dibenzo[b,d]pyran-1-yl]oxy}butan-2-yl]amino}-4-oxobutanoic acid 3-{[(2S)-1-{[(6aR,10aR)-6,6,9-trimethyl-3-pentyl-6H,6aH,7H,8H,10aH-benzo[c]isochromen-1-yl]oxy}-3-methyl-1-oxobutan-2-yl]carbamoyl}propanoic acid 4-{[(2S)-3-methyl-1-oxo-1-{[(6aR,10aR)-6,6,9-trimethyl-3-pentyl-6a,7,8,10a-tetrahydro-6H-dibenzo[b,d]pyran-1-yl]oxy}butan-2-yl]amino}-4-oxobutanoic acidcannabinoid receptor agonist, DB 21741, XV9S3R9XJC Suvadronabinol (DB21741) is a potent, synthetic small-molecule cannabinoid receptor type 1 (CB1) agonist, initially developed for therapeutic potential in areas like appetite stimulation, pain, or weight management, acting similarly to cannabis compounds but with …

Surzetoclax

It’s only fair to share… Surzetoclax CAS 2858632-01-4 MF C53H63ClN8O10S, 1039.64 NAMES 4-[(4aS,10aR)-14-(4-chlorophenyl)-12,12-dimethyl1,2,4a,5,8,9,10a,11,13,15-decahydro-7H,12Hpyrazino[2,1-g][1,5,8]benzodioxaazacycloundecin3(4H)-yl]-2-(3,4-dihydro-2Hpyrrolo[3′,2′:5,6]pyrido[2,3-b][1,4]oxazepin-1(7H)-yl)-N-[4-({[(2S,5R)-5-methoxyoxan-2-yl]methyl}amino)-3-nitrobenzene-1-sulfonyl]benzamide 4-(14-(4-chlorophenyl)-12,12-dimethyl-1,2,4a,5,8,9,10a,11,13,15-decahydro-7H,12H-benzo[f]pyrazino[2,1-c][1,8]dioxa[4]azacycloundecin-3(4H)-yl)-2-(3,4-dihydro-2H-pyrrolo[3′,2′:5,6]pyrido[2,3-b][1,4]oxazepin-1(7H)-yl)-N-((4-((((2S,5R)-5-methoxytetrahydro-2H-pyran-2-yl)methyl)amino)-3-nitrophenyl)sulfonyl)benzamide D-erythro-Hexitol, 1,5-anhydro-6-[[4-[[[4-[(4aS,10aR)-14-(4-chlorophenyl)-1,2,4a,5,8,9,10a,11,13,15-decahydro-12,12-dimethyl-7H,12H-pyrazino[2,1-g][1,5,8]benzodioxaazacycloundecin-3(4H)-yl]-2-(3,4-dihydro-2H-pyrrolo[3′,2′:5,6]pyrido[2,3-b][1,4]oxazepin-1(7H)-yl)benzoyl]amino]sulfonyl]-2-nitrophenyl]amino]-3,4,6-trideoxy-2-O-methyl- 1,5-Anhydro-6-[[4-[[[4-[(4aS,10aR)-14-(4-chlorophenyl)-1,2,4a,5,8,9,10a,11,13,15-decahydro-12,12-dimethyl-7H,12H-pyrazino[2,1-g][1,5,8]benzodioxaazacycloundecin-3(4H)-yl]-2-(3,4-dihydro-2H-pyrrolo[3′,2′:5,6]pyrido[2,3-b][1,4]oxazepin-1(7H)-yl)benzoyl]amino]sulfonyl]-2-nitrophenyl]amino]-3,4,6-trideoxy-2-O-methyl-D-erythro-hexitolB-cell lymphoma 2 (Bcl-2) inhibitor, antineoplastic, ABBV 453, C3TU3CHH6L, Bcl-2-IN-16 Surzetoclax, also known as ABBV 453; is a highly potent and selective BCL-2 inhibitor with a Ki of approximately 0.07 nM. It induces apoptosis in BCL-2–dependent hematologic cancer cells, …