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1204975-42-7

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  • 2-PYRAZINEMETHANOL, 5-[(2R)-4-[4,5-DIMETHYL-6-(PHENYLMETHYL)-3-PYRIDAZINYL]-2-METHYL-1-PIPERAZINYL]-ALPHA,ALPHA-DIMETHYL-

    Cas No: 1204975-42-7

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1204975-42-7 Usage

Description

LEQ-506 is a second-generation inhibitor of smoothened (Smo) protein, which is a key component in the Hedgehog signaling pathway. It has demonstrated potent inhibitory activity with IC50s of 2 and 4 nM in human and mouse, respectively. This makes LEQ-506 a promising candidate for therapeutic applications targeting the Hedgehog signaling pathway.

Uses

Used in Pharmaceutical Industry:
LEQ-506 is used as a therapeutic agent for targeting the Hedgehog signaling pathway, which plays a crucial role in various cellular processes, including embryonic development, tissue regeneration, and stem cell maintenance. Dysregulation of this pathway has been associated with several cancers and congenital disorders, making LEQ-506 a potential treatment option for such conditions.
Used in Cancer Treatment:
LEQ-506 is used as an anticancer agent, particularly in the treatment of tumors that rely on the aberrant activation of the Hedgehog signaling pathway for growth and survival. By inhibiting the Smo protein, LEQ-506 can potentially halt tumor progression and improve patient outcomes in various cancer types.
Used in Drug Development:
LEQ-506 is used as a lead compound in the development of novel therapeutics targeting the Hedgehog signaling pathway. Its potent inhibitory activity and selectivity make it a valuable starting point for designing new drugs with improved efficacy, safety, and pharmacokinetic properties.
Used in Research Applications:
LEQ-506 is used as a research tool for studying the role of the Hedgehog signaling pathway in various biological processes and disease states. Its ability to selectively inhibit the Smo protein allows researchers to investigate the molecular mechanisms underlying Hedgehog-mediated cellular responses and identify potential therapeutic targets for intervention.

Check Digit Verification of cas no

The CAS Registry Mumber 1204975-42-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,0,4,9,7 and 5 respectively; the second part has 2 digits, 4 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1204975-42:
(9*1)+(8*2)+(7*0)+(6*4)+(5*9)+(4*7)+(3*5)+(2*4)+(1*2)=147
147 % 10 = 7
So 1204975-42-7 is a valid CAS Registry Number.

1204975-42-7Relevant articles and documents

Discovery of NVP-LEQ506, a second-generation inhibitor of smoothened

Peukert, Stefan,He, Feng,Dai, Miao,Zhang, Rui,Sun, Yingchuan,Miller-Moslin, Karen,Mcewan, Michael,Lagu, Bharat,Wang, Kate,Yusuff, Naeem,Bourret, Aaron,Ramamurthy, Arun,Maniara, Wieslawa,Amaral, Adam,Vattay, Anthony,Wang, Anlai,Guo, Ribo,Yuan, Jing,Green, John,Williams, Juliet,Buonamici, Silvia,Kelleher, Joseph F.,Dorsch, Marion

, p. 1261 - 1265 (2013/08/23)

First disclosure: Continued optimization provided a novel type of Smoothened (Smo) antagonist based on a pyridazine core. The compound, NVP-LEQ506, currently in phaseI clinical trials, combines high intrinsic potency and good pharmacokinetic properties resulting in excellent efficacy in rodent tumor models of medulloblastoma. Activity against a Smo mutant conferring resistance observed in a previous clinical trial with a competitor compound suggests additional therapeutic potential.

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