General Information of the Drug (ID: M6APDG00337)
Name
AZD8931
Synonyms
Sapitinib; AZD8931; 848942-61-0; AZD8931 (Sapitinib); AZD-8931; Sapitinib(AZD8931); UNII-3499328002; CHEMBL2408045; 2-(4-((4-((3-Chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)-n-methylacetamide; 2-[4-({4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl}oxy)piperidin-1-yl]-N-methylacetamide; Sapitinib [INN]; 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-((1-(n-methylcarbamoylmethyl)piperidin-4-yl)oxy)quinazoline
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Status
Phase 2
Structure
Formula
C23H25ClFN5O3
InChI
1S/C23H25ClFN5O3/c1-26-21(31)12-30-8-6-14(7-9-30)33-20-10-15-18(11-19(20)32-2)27-13-28-23(15)29-17-5-3-4-16(24)22(17)25/h3-5,10-11,13-14H,6-9,12H2,1-2H3,(H,26,31)(H,27,28,29)
InChIKey
DFJSJLGUIXFDJP-UHFFFAOYSA-N
PubChem CID
11488320
TTD Drug ID
D0BM7M
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.
Erbb2 tyrosine kinase receptor (HER2)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Erbb2 tyrosine kinase receptor (HER2) is a therapeutic target for AZD8931. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of AZD8931 through regulating the expression of Erbb2 tyrosine kinase receptor (HER2). [1], [2]
Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2)
In total 1 mechanisms lead to this potential drug response
Response Summary Erbb2 tyrosine kinase receptor (HER2) is a therapeutic target for AZD8931. The Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2) has potential in affecting the response of AZD8931 through regulating the expression of Erbb2 tyrosine kinase receptor (HER2). [2], [3]
References
Ref 1 FTO mediated ERBB2 demethylation promotes tumor progression in esophageal squamous cell carcinoma cells. Clin Exp Metastasis. 2022 Aug;39(4):623-639. doi: 10.1007/s10585-022-10169-4. Epub 2022 May 7.
Ref 2 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
Ref 3 IGF2BP2 promotes the progression of colorectal cancer through a YAP-dependent mechanism. Cancer Sci. 2021 Oct;112(10):4087-4099. doi: 10.1111/cas.15083. Epub 2021 Aug 3.