Drug Details

General Information of the Drug (ID: DR9224)
Name
BI-D1870
Synonyms
BI-D1870; 501437-28-1; 2-((3,5-difluoro-4-hydroxyphenyl)amino)-8-isopentyl-5,7-dimethyl-7,8-dihydropteridin-6(5H)-one; 2-(3,5-difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7H-pteridin-6-one; C19H23F2N5O2; 2-((3,5-difluoro-4-hydroxyphenyl)amino)-8-isopentyl-5,7-dimethyl-7,8-dihydropteridin-6(5H)-one.; 2-(3,5-difluoro-4-hydroxyphenylamino)-8-isopentyl-5,7-dimethyl-7,8-dihydropteridin-6(5H)-one; 2-[(3,5-DIFLUORO-4-HYDROXYPHENYL)AMINO]-7,8-DIHYDRO-5,7-DIMETHYL-8-(3-METHYLBUTYL)-6(5H)-PTERIDINONE; cc-687; CHEMBL573107; GTPL8038; SCHEMBL13881333; BDBM25017; BID1870; DTXSID40648506; SYN1020; BCPP000343; HMS3244C11; HMS3244C12; HMS3244D11; HMS3651D17; HMS3674C15; BCP01977; EX-A2471; ABP000282; BI-D-1870; MFCD11223662; NSC747342; s2843; AKOS015918879; BCP9000401; CCG-268540; CS-1243; NSC-747342; SB19282; AC-32826; AK-37190; AS-16192; HY-10510; AB0007926; DB-071116; FT-0720677; SW219252-1; X5923; W-5481; 437D281; J-505744; Q27075243; 2-(3,5-Difluoro-4-hydroxy-phenylamino)-5,7-dimethyl-8-(3-methyl-butyl)-7,8-dihydro-5H-pteridin-6-one; 2-(3,5-Difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7,8-dihydropteridin-6(5H)-one; 2-(3,5-difluoro-4-hydroxyphenylamino)-8-isopentyl-5,7-dimethyl-7,8-dihydropyrido[2,3-d]pyrimidin-6(5H)-one; 2-[(3,5-difluoro-4-hydroxyphenyl)amino]-5,7-dimethyl-8-(3-methylbutyl)-5,6,7,8-tetrahydropteridin-6-one; 2-[(3,5-Difluoro-4-hydroxyphenyl)amino]-5,7-dimethyl-8-(3-methylbutyl)-7,8-dihydropteridin-6(5H)-one; 2-[(3,5-difluoro-4-hydroxyphenyl)amino]-7,8-dihydro-5,7-dimethyl-8-(3-methylbutyl)-6(5h)-pteridone
    Click to Show/Hide
Molecular Type
Small molecule
Disease Chronic lymphocytic leukaemia [ICD-11: 2A82] Preclinical [1]
Structure
Click to Download Mol
2D MOL

3D MOL

    Click to Show/Hide the Molecular Information and External Link(s) of This Natural Product
Formula
C19H23F2N5O2
PubChem CID
25023738
Canonical SMILES
CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C
InChI
1S/C19H23F2N5O2/c1-10(2)5-6-26-11(3)18(28)25(4)15-9-22-19(24-17(15)26)23-12-7-13(20)16(27)14(21)8-12/h7-11,27H,5-6H2,1-4H3,(H,22,23,24)
InChIKey
DTEKTGDVSARYDS-UHFFFAOYSA-N
CAS Number
CAS 501437-28-1
TTD Drug ID
D02VBF
Combinatorial Therapeutic Effect(s) Validated Clinically or Experimentally
    α. A List of Natural Product(s) Able to Enhance the Efficacy of This Drug
          Vincristine      Catharanthus roseus     Click to Show/Hide the Molecular Data of This NP
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [2]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Biological
                    Regulation		 Induction Cell cycle arrest in M phase
                    In-vitro Model KG-1 CVCL_0374 Adult acute myeloid leukemia Homo sapiens
HL-60 CVCL_0002 Adult acute myeloid leukemia Homo sapiens
NALM-6 CVCL_0092 Adult B acute lymphoblastic leukemia Homo sapiens
                    Experimental
                    Result(s)		 BI-D1870 induces apoptosis of AML cells alone and in combination with vincristine through blocking mitotic exit, providing a novel approach to overcoming vincristine resistance in AML cells.
Target and Pathway
Target(s) Ribosomal protein S6 kinase alpha-1 (RSK1)  Molecule Info  [1]
Ribosomal protein S6 kinase alpha-2 (RSK2)  Molecule Info  [1]
Ribosomal protein S6 kinase alpha-3 (RSK3)  Molecule Info  [1]
Ribosomal protein S6 kinase alpha-6 (RSK6)  Molecule Info  [1]
References
Reference 1 BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem J. 2007 Jan 1;401(1):29-38.
Reference 2 RSK inhibitor BI-D1870 inhibits acute myeloid leukemia cell proliferation by targeting mitotic exit. Oncotarget. 2020 Jun 23;11(25):2387-2403.
 Download Picture         KEGG Link