Sunan samfur:1- (methylsulfonyl) spiro [indoline-3,Wani Suna: 1,2-dihydro-1- (methylsulfonyl) -Spiro [3H-indole-3,4'-piperidine]; Spiro [3H-indole-3,4'-piperidine], 1,2-dihydro-1- (methylsulfonyl) -; 1-methylsulfonylspiro [2H-indole-pipe-3,4]

CAS NO.:178261-41-1

Matsayi: 98.0%

Launi: kashe-fari foda

Shiryawa:25kg/DRUMS

1- (Methylsulfonyl) spiro [indoline-3,4'-piperidine]: Mai iya hana c-Met / ALK Dual Inhibitor don Binciken Oncology

Bayanin Samfura

1-(Methylsulfonyl) spiro [indoline-3,4'-piperidine] (CAS: 178261-41-1) wani fili ne na spirocyclic tare da tsarin kwayoyin C₁₃H₁₉ ClN₂O₂S da nauyin kwayoyin halitta na 302.83. Wannan babban-tsarki (> 95%) ƙananan kwayoyin halitta an gane shi don maɗaukakin gata a cikin ƙirar kinase inhibitor, musamman maƙasudin c-Met (mai karɓar haɓakar haɓakar hepatocyte) da ALK (anaplastic lymphoma kinase), direbobin oncogenic guda biyu masu mahimmanci a cikin ciwon daji.

Ayyukan Pharmacological & Aikace-aikace

1. Dual c-Met / ALK hanawa

Matsakaicin spiro [indoline-3,4′-piperidine] yana ba da damar hanawa mai ƙarfi da zaɓi na c-Met da ALK kinases. Nazarin preclinical ya nuna:

• Ƙarfin sinadarai masu lamba ɗaya nM akan c-Met da ALK .
• In vivo inganci a cikin murkushe haɓakar ƙari (> 50% hanawa) a cikin ƙwayoyin cuta na ciki na xenograft.
• Halin halittu na baka da ingantattun magunguna, yana sa ya dace da haɓakar warkewa.

2. Tsarin Aiki (MoA)

Ƙungiyar methylsulfonyl tana haɓaka solubility da haɗin kai, yayin da tsarin spiro yana ba da damar hulɗar da aka fallasa da ƙarfi tare da yankunan kinase, yana rage tasirin kashe-kashe. An tabbatar da wannan zaɓin ta hanyar nunin panel 97-kinase, inda fili ya nuna ƙarancin amsawar giciye.

3. Yiwuwar warkewa

• Yana nufin ciwon daji tare da dysregulated c-Met / ALK siginar, ciki har da wadanda ba kananan cell huhu ciwon daji (NSCLC), na ciki carcinoma, da glioblastoma.
• Yana aiki azaman tsaka-tsaki na sinadarai don haɓaka analogs tare da ingantattun bayanan martaba na pharmacokinetic .Synthesis & Quality Assurance

1. Ingantattun Hanyoyi na roba

• Halayen sassa huɗu waɗanda suka haɗa da isatin, methyl propiolate, da arylamines suna samar da spiro mai aiki [indoline-3,4'-piperidine] tare da babban regioselectivity.
• Haɗin Suzuki da halayen Mitsunobu suna ba da damar aiki na yau da kullun na ainihin tsarin don analogs iri-iri.

2. Quality Control

An ba da shi ta hanyar masana'anta masu dogaro (misali, Bellingham & Stanley, Matrix Scientific), samfurin yana fuskantar tsauraran HPLC da tabbaci na NMR don tabbatar da tsabtar ≥95%.

Taimakon Bincike & Bayani

• Mabuɗin Mahimmanci: Docking Kwayoyin Halitta: Nazarin tsarin yana tabbatar da hulɗa tare da yankunan kinase hinge, yana goyan bayan ƙirar ƙwayoyi masu ma'ana.
  • Li et al. (2013) gano spiro [indoline-3,4'-piperidine] -2-waɗanda a matsayin masu hana c-Met / ALK masu zaɓi.
  • Zhang et al. (2013) ya haɓaka ƙirar tukunya ɗaya don mahaɗan spiro, yana nuna hanyoyin haɓaka.

Kammalawa

1- (Methylsulfonyl) spiro [indoline-3,4'-piperidine] ɗan takara ne mai ban sha'awa don bincike na oncology, haɗa babban zaɓi, ingancin baka, da samun damar roba. Aikace-aikacen sa sun taso daga haɓaka mahaɗan gubar zuwa nazarin injiniyoyi a cikin cututtukan da ke haifar da kinase.

Bayanin mai bayarwa

• CAS: 178261-41-1 | Tsafta:> 95%
• Samuwar: Masu samar da kayayyaki na duniya (misali, ChemNet, Bellingham & Stanley) ne.
• Contact: info@trbextract.com 

Mahimman kalmomi: c-Met inhibitor, ALK inhibitor, spiro [indoline-3,4'-piperidine], kinase inhibitor synthesis, oncology bincike mahadi.