SML2608
CSRM617 Hydrochloride
≥98% (HPLC)
别名:
(2,3,4-Trihydroxyphenyl-methylidene)-hydrazino-2-amino-3-hydroxy-1-propanone hydrochloride, 2-Amino-3-hydroxy-N′-(2,3,4-trihydroxybenzylidene)propanehydrazide hydrochloride, 2-[(2,3,4-trihydroxyphenyl)methylene] serinehydrazide hydrochloride (1:1)
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About This Item
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化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
white to beige
溶解度
H2O: 2 mg/mL, clear
儲存溫度
−20°C
SMILES 字串
OC1=C(C=CC(O)=C1O)C=NNC(C(CO)N)=O.Cl
生化／生理作用
CSRM617 is an ONECUT2 (OC2) inhibitor that directly targets OC2 HOX domain (KD = 7.43 μM) and disrupts OC2 target genes promoter binding. CSRM617 blocks OC2-dependent prostate cancer growth in cultures (IC50 = 4-50 μM; 48 h) via apoptosis induction (fold of untreated annexin V population = 2.3/10 μM, 3.5/20 μM; 22Rv1) and exhibits in vivo efficacy against metastases as well as the growth of established 22Rv1 tumor in mice in vivo (50 mg/kg/day ip.).
訊號詞
Warning
危險分類
Aquatic Acute 1 - Aquatic Chronic 1 - Eye Irrit. 2 - Muta. 2 - Skin Sens. 1
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Irene Zamora et al.
Cellular oncology (Dordrecht, Netherlands) (2024-05-31)
Tumor heterogeneity complicates patient treatment and can be due to transitioning of cancer cells across phenotypic cell states. This process is associated with the acquisition of independence from an oncogenic driver, such as the estrogen receptor (ER) in breast cancer
Mirja Rotinen et al.
Nature medicine, 24(12), 1887-1898 (2018-11-28)
Treatment of prostate cancer (PC) by androgen suppression promotes the emergence of aggressive variants that are androgen receptor (AR) independent. Here we identify the transcription factor ONECUT2 (OC2) as a master regulator of AR networks in metastatic castration-resistant prostate cancer
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