Thalidomide

Sharaxaad Gaaban:

Magaca API Tilmaan Tilmaamid US DMF Midowga Yurub DMF CEP
Thalidomide Daawooyinka Oncology USP/EP      


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Asalkii hore

Thalidomide waxaa loo soo bandhigay dawo dejineed, wakiilka immunomodulatory iyo sidoo kale waxaa lagu baarayaa daaweynta calaamadaha kansarrada badan. Thalidomide wuxuu joojiyaa E3 ubiquitin ligase,kaas oo ah CRBN-DDB1-Cul4A.

Sharaxaada

Thalidomide waxaa markii hore loo dallacsiiyay sidii dawo dejineed, waxay joojisaa cereblon (CRBN), qayb ka mid ah cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, oo leh Kd of250 nM, oo uu leeyahay difaaca jirka, anti-bararka iyo sifooyinka kansarka angiogenic.

In Vitro

Thalidomide ayaa markii hore loo dallacsiiyay sidii dawo dejineed, waxay leedahay immunomodulatory, anti-bararka iyo guryaha kansarka anti-angiogenic, iyo bartilmaameedyada cereblon (CRBN), qayb ka mid ah cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, oo leh Kd of250 nM[1]. Thalidomide (50μg / mL) waxay xoojisaa dhaqdhaqaaqa ka hortagga burooyinka ee icotinib oo ka soo horjeeda faafitaanka unugyada PC9 iyo A549 labadaba, saameyntani waxay la xiriirtaa apoptosis iyo socdaalka unugyada. Intaa waxaa dheer, Thalidomide iyo icotinib waxay joojinayaan waddooyinka EGFR iyo VEGF-R2 ee unugyada PC9[3].

Thalidomide (100 mg / kg, po) waxay joojisaa dhigaalka kolajka, waxay hoos u dhigtaa heerka muujinta mRNAα-SMA iyo collagen I, waxayna si weyn u yaraynaysaa cytokines-ka-bararka ee jiirarka RILF. Thalidomide waxay yaraynaysaa RILF iyada oo loo marayo xakamaynta ROS iyo hoos u dhigista TGF-β/ Dariiqa Smad waxay kuxirantahay heerka Nrf2[2]. Thalidomide (200 mg/kg, po) oo ay weheliso icotinib waxay muujinaysaa saamaynta ka hortagga burooyinka ee jiirarka qaawan ee wata unugyada PC9, xakamaynta koritaanka burada iyo kor u qaadida dhimashada burooyinka[3].

Kaydinta

Budada

-20°C

3 sano

4°C

2 sano
Ku milmay

-80°C

6 bilood

-20°C

1 bil

Qaab dhismeedka kiimikada

Thalidomide

SHAHAADADA

2018 GMP-2
原料药GMP证书201811 (captopril, thalidomide iwm)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

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