General Information of the Drug (ID: M6APDG03037)
Name
BVB-808
Synonyms
JAK2 tyrosine kinase inhibitors (cancer), Novartis; NVP-BSK-805
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Status
Investigative
Structure
Formula
C29H33F2N7O
InChI
1S/C29H33F2N7O/c1-19-16-37(17-20(2)33-19)23-5-3-22(4-6-23)34-29-32-15-21-7-8-38(28(21)35-29)24-13-26(30)25(27(31)14-24)18-36-9-11-39-12-10-36/h3-8,13-15,19-20,33H,9-12,16-18H2,1-2H3,(H,32,34,35)/t19-,20+
InChIKey
VIIPVCPPCBLRRL-BGYRXZFFSA-N
PubChem CID
90480481
TTD Drug ID
D0N8CN
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.
Janus kinase 2 (JAK-2)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Janus kinase 2 (JAK-2) is a therapeutic target for BVB-808. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of BVB-808 through regulating the expression of Janus kinase 2 (JAK-2). [1], [2]
Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1)
In total 1 mechanisms lead to this potential drug response
Response Summary Janus kinase 2 (JAK-2) is a therapeutic target for BVB-808. The Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1) has potential in affecting the response of BVB-808 through regulating the expression of Janus kinase 2 (JAK-2). [2], [3]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Janus kinase 2 (JAK-2) is a therapeutic target for BVB-808. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of BVB-808 through regulating the expression of Janus kinase 2 (JAK-2). [2], [3]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
Response Summary Janus kinase 2 (JAK-2) is a therapeutic target for BVB-808. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of BVB-808 through regulating the expression of Janus kinase 2 (JAK-2). [2], [4]
References
Ref 1 FTO inhibits UPR(mt)-induced apoptosis by activating JAK2/STAT3 pathway and reducing m6A level in adipocytes. Apoptosis. 2021 Aug;26(7-8):474-487. doi: 10.1007/s10495-021-01683-z. Epub 2021 Jul 1.
Ref 2 Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2. J Biol Chem. 2008 Nov 21;283(47):32334-43. doi: 10.1074/jbc.M803813200. Epub 2008 Sep 4.
Ref 3 N6-Methyladenosine Methyltransferase METTL3 Promotes Angiogenesis and Atherosclerosis by Upregulating the JAK2/STAT3 Pathway via m6A Reader IGF2BP1. Front Cell Dev Biol. 2021 Dec 7;9:731810. doi: 10.3389/fcell.2021.731810. eCollection 2021.
Ref 4 ALKBH5-HOXA10 loop-mediated JAK2 m6A demethylation and cisplatin resistance in epithelial ovarian cancer. J Exp Clin Cancer Res. 2021 Sep 8;40(1):284. doi: 10.1186/s13046-021-02088-1.