General Information of the Drug (ID: M6APDG03339)
Name
INK128
Synonyms
1224844-38-5; Sapanisertib; INK-128; INK 128; INK 128 (MLN0128); TAK-228; UNII-JGH0DF1U03; JGH0DF1U03; 5-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)benzo[d]oxazol-2-amine; INK-0128; 3-(2-Amino-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; C15H15N7O; 5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine; 5-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]-pyrimidin-3-yl)benzo[d]oxazol-2-amine; Sapanisertib (USAN/INN)
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Status
Phase 2
Structure
Formula
C15H15N7O
InChI
1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19)
InChIKey
GYLDXIAOMVERTK-UHFFFAOYSA-N
PubChem CID
45375953
TTD Drug ID
D03DPZ
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Serine/threonine-protein kinase mTOR (mTOR)
Fat mass and obesity-associated protein (FTO)
In total 2 mechanisms lead to this potential drug response
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for INK128. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of INK128 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [1], [2]
Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for INK128. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of INK128 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [1], [3]
Methyltransferase-like 14 (METTL14)
In total 2 mechanisms lead to this potential drug response
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for INK128. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of INK128 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [2], [4]
Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for INK128. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of INK128 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [3], [4]
Methyltransferase-like 3 (METTL3)
In total 2 mechanisms lead to this potential drug response
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for INK128. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of INK128 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [2], [5]
Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for INK128. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of INK128 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [3], [5]
YTH domain-containing family protein 1 (YTHDF1)
In total 2 mechanisms lead to this potential drug response
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for INK128. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of INK128 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [2], [6]
Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for INK128. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of INK128 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [3], [6]
YTH domain-containing family protein 2 (YTHDF2)
In total 2 mechanisms lead to this potential drug response
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for INK128. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of INK128 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [1], [2]
Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for INK128. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of INK128 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [1], [3]
References
Ref 1 Targeting ATF4-dependent pro-survival autophagy to synergize glutaminolysis inhibition. Theranostics. 2021 Jul 25;11(17):8464-8479. doi: 10.7150/thno.60028. eCollection 2021.
Ref 2 Dramatic suppression of colorectal cancer cell growth by the dual mTORC1 and mTORC2 inhibitor AZD-2014. Biochem Biophys Res Commun. 2014 Jan 10;443(2):406-12. doi: 10.1016/j.bbrc.2013.11.099. Epub 2013 Dec 2.
Ref 3 Genta obtains orphan drug designation for C-Myb Antisense (LR3001) in chronic myelocytic leukemia. Genta. 2005.
Ref 4 The m6A methyltransferase METTL14 inhibits the proliferation, migration, and invasion of gastric cancer by regulating the PI3K/AKT/mTOR signaling pathway. J Clin Lab Anal. 2021 Mar;35(3):e23655. doi: 10.1002/jcla.23655. Epub 2020 Dec 12.
Ref 5 Methyltransferase-like 3 promotes the progression of lung cancer via activating PI3K/AKT/mTOR pathway. Clin Exp Pharmacol Physiol. 2022 Jul;49(7):748-758. doi: 10.1111/1440-1681.13647. Epub 2022 May 23.
Ref 6 YTHDF1 promotes hepatocellular carcinoma progression via activating PI3K/AKT/mTOR signaling pathway and inducing epithelial-mesenchymal transition. Exp Hematol Oncol. 2021 Jun 4;10(1):35. doi: 10.1186/s40164-021-00227-0.