221243-77-2 Usage
Description
4-Amino-1-tert-butyl-3-(1'-naphthylmethyl)-4-cyanopyrazole is a chemical compound characterized by its unique molecular structure, which features a pyrazole core with various functional groups attached. 4-Amino-1-tert-butyl-3-(1'-naphthylmethyl)-4-cyanopyrazole is known for its potent and specific inhibitory activity against tyrosine kinases, particularly a rationally engineered v-Src tyrosine kinase.
Uses
Used in Pharmaceutical Industry:
4-Amino-1-tert-butyl-3-(1'-naphthylmethyl)-4-cyanopyrazole is used as a tyrosine kinase inhibitor for its high potency (IC50=1.5nM) and unique specificity. This makes it a valuable compound in the development of targeted therapies for various diseases, particularly those involving abnormal tyrosine kinase activity, such as certain types of cancer.
Used in Cancer Research:
In the field of cancer research, 4-Amino-1-tert-butyl-3-(1'-naphthylmethyl)-4-cyanopyrazole serves as a valuable tool for studying the role of tyrosine kinases in cancer cell growth and proliferation. Its high potency and specificity allow researchers to investigate the molecular mechanisms underlying cancer development and progression, potentially leading to the discovery of novel therapeutic strategies.
Used in Drug Development:
4-Amino-1-tert-butyl-3-(1'-naphthylmethyl)-4-cyanopyrazole is used as a lead compound in the development of new drugs targeting tyrosine kinases. Its unique properties make it an attractive starting point for the design and synthesis of more potent and selective inhibitors, which could be used in the treatment of various diseases, including cancer and other conditions characterized by dysregulated tyrosine kinase activity.
Check Digit Verification of cas no
The CAS Registry Mumber 221243-77-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,2,1,2,4 and 3 respectively; the second part has 2 digits, 7 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 221243-77:
(8*2)+(7*2)+(6*1)+(5*2)+(4*4)+(3*3)+(2*7)+(1*7)=92
92 % 10 = 2
So 221243-77-2 is a valid CAS Registry Number.
InChI:InChI=1/C19H20N4/c1-19(2,3)23-18(21)16(12-20)17(22-23)11-14-9-6-8-13-7-4-5-10-15(13)14/h4-10H,11,21H2,1-3H3
221243-77-2Relevant articles and documents
Discovery of a potent protein kinase D inhibitor: insights in the binding mode of pyrazolo[3,4-d]pyrimidine analogues
Verschueren, Klaas,Cobbaut, Mathias,Demaerel, Joachim,Saadah, Lina,Voet, Arnout R. D.,Van Lint, Johan,De Borggraeve, Wim M.
, p. 640 - 646 (2017/03/30)
In this study, we set out to rationally optimize PKD inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold. The lead compound for this study was 1-NM-PP1, which was previously found by us and others to inhibit PKD. In our screening we identified one compound (3-IN-PP1) displaying a 10-fold increase in potency over 1-NM-PP1, opening new possibilities for specific protein kinase inhibitors for kinases that show sensitivity towards pyrazolo[3,4-d]pyrimidine derived compounds. Interestingly the observed SAR was not in complete agreement with the commonly observed binding mode where the pyrazolo[3,4-d]pyrimidine compounds are bound in a similar fashion as PKD's natural ligand ATP. Therefore we suggest an alternate binding mode where the compounds are flipped 180 degrees. This possible alternate binding mode for pyrazolo[3,4-d]pyrimidine based compounds could pave the way for a new class of specific protein kinase inhibitors for kinases sensitive towards pyrazolo[3,4-d]pyrmidines.
Generation of monospecific nanomolar tyrosine kinase inhibitors via a chemical genetic approach
Bishop, Anthony C.,Kung, Chi-Yun,Shah, Kavita,Witucki, Laurie,Shokat, Kevan M.,Liu, Yi
, p. 627 - 631 (2007/10/03)
Selective protein kinase inhibitors are highly sought after as tools for studying cellular signal transduction cascades, yet few have been discovered due to the highly conserved fold of kinase catalytic domains. Through a combination of small molecule syn
