37854-59-4 Usage
Uses
Ro 08-2750 is a TrkA inhibitor and NGF-induced apoptosis inhibitor.
Biological Activity
Non-peptide inhibitor of NGF that binds the NGF dimer (K D ~ 1 μ M) possibly causing a conformational change. Inhibits binding selectively to p75 NTR at submicromolar concentrations and to both p75 NTR and TrkA at higher concentrations (> 5 μ M). Prevents NGF-induced apoptosis in SK-N-MC cells.
in vitro
ro 08-2750 can bind to the ngf dimer with ~ 1:1 binding ratio. binding of ro 08-2750 to ngf induces ngf a concentration-dependent conformational change [1]. binding with low concentration of ro 08-2750, ngf can no longer bind to p75ntr anymore, however, binding to trka is not impaired. at higher concentrations of ro 08-2750 more than 5 mm, the ngf/ro 08-2750 complex can not bind to trka as well. in sk-n-mc cells, ro 08-2750 leads to inhibition of ngf-induced programmed cell death. in pc12 cells, ro 08-2750 can enhance the signal pathway through trka[2].
IC 50
1 μm (binds to ngf) [1]
references
[1] arkin mr, wells ja. small-molecule inhibitors of protein-protein interactions: progressing towards the dream. nat rev drug discov. 2004 apr;3(4):301-17.[2] niederhauser o, mangold m, schubenel r, kusznir ea, schmidt d, hertel c. ngf ligand alters ngf signaling via p75(ntr) and trka. j neurosci res. 2000 aug 1;61(3):263-72.
Check Digit Verification of cas no
The CAS Registry Mumber 37854-59-4 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 3,7,8,5 and 4 respectively; the second part has 2 digits, 5 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 37854-59:
(7*3)+(6*7)+(5*8)+(4*5)+(3*4)+(2*5)+(1*9)=154
154 % 10 = 4
So 37854-59-4 is a valid CAS Registry Number.
InChI:InChI=1/C13H10N4O3/c1-6-3-8-9(4-7(6)5-18)17(2)11-10(14-8)12(19)16-13(20)15-11/h3-5H,1-2H3,(H,16,19,20)
37854-59-4Relevant articles and documents
PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER CONTAINING PLK1 INHIBITOR AS ACTIVE INGREDIENT
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, (2022/02/11)
The present invention relates to a pharmaceutical composition for preventing, treating or alleviating cancer, containing a PLK1 inhibitor as an active ingredient, and a compound according to the present invention selectively binds to PBD of PLK1, thereby having advantages of high selectivity and binding affinity for PLK1 and low toxicity. Therefore, a PLK inhibitor compound according to the present invention can be effectively used as an anticancer agent by inhibiting the growth of various cancer cells, and can be expected to exhibit synergistic effects with existing developed anticancer agents through co-administration, in addition to individual administration thereof.
