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产品名称
A 83-01, ≥98% (HPLC)
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 5 mg/mL, clear (warmed)
储存温度
−20°C
SMILES字符串
S=C([n]2nc(c(c2)c4c5c(ncc4)cccc5)c3nc(ccc3)C)Nc1ccccc1
InChI
1S/C25H19N5S/c1-17-8-7-13-23(27-17)24-21(19-14-15-26-22-12-6-5-11-20(19)22)16-30(29-24)25(31)28-18-9-3-2-4-10-18/h2-16H,1H3,(H,28,31)
InChI key
HIJMSZGHKQPPJS-UHFFFAOYSA-N
一般描述
A-83-01可有效抑制烧伤创面收缩而不影响创面愈合，因为它可抑制转化生长因子-β (TGF-β)诱导的肌成纤维细胞群增加。此外，还可通过抑制动物的上皮间质转化(EMT)来阻止TGF-β1-依赖的癌症转移。
应用
A 83-01已用于：
- 加入培养基用于分离肿瘤细胞的类器官形成，
- 加入杜氏改良Eagle培养基/F-12营养混合物(DMEM/F12)中以培养人表皮干细胞(EpSCs)
A 83-01已被用作转化生长因子β激酶1型受体的抑制剂。
生化/生理作用
A 83-01是一种TGFβ激酶/激活素受体样激酶（ALK 5）的抑制剂（IC50= 12nM），可阻止Smad2/3的磷酸化并抑制TGFβ诱导的生长。 A 83-01可阻断Smad2的磷酸化并抑制TGF-β诱导的上皮-间质转化。 此外，A 83-01可抑制由TGFβI型受体ALK-5、活化素IB型受体ALK-4、和结节型I受体ALK-7诱导的转录活性。 A-83-01可诱导新生Nkx2.5-eGFP（+）细胞的扩增。
A-83-01是一种TGFβ激酶/激活素受体样激酶(ALK 5)抑制剂。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
A83-01 inhibits TGF-Β-induced upregulation of Wnt3 and epithelial to mesenchymal transition in HER2-overexpressing breast cancer cells.
Wu Y, et al.
Breast Cancer Research and Treatment, 163(3), 449-460 (2017)
The Use of Endometrial Cancer Patient?Derived Organoid Culture for Drug Sensitivity Testing Is Feasible
Girda E, et al.
International Journal of Gynecological Cancer : Official Journal of the International Gynecological Cancer Society, 27(8), 1701-1701 (2017)
Topical application of ALK5 inhibitor A-83-01 reduces burn wound contraction in rats by suppressing myofibroblast population
Sun X, et al.
Bioscience, Biotechnology, and Biochemistry, 78, 1805-1812 (2014)
Personalized identification of optimal HIPEC perfusion protocol in patient-derived tumor organoid platform
Forsythe SD, et al.
Annals of Surgical Oncology, 27, 4950-4960 (2020)
Eugenia Girda et al.
International journal of gynecological cancer : official journal of the International Gynecological Cancer Society, 27(8), 1701-1707 (2017-07-07)
Patient-derived organoids (PDOs), used in multiple tumor types, have allowed evaluation of tumor characteristics from individual patients. This study aimed to assess the feasibility of applying PDO in vitro culture for endocrine-based and drug sensitivity testing in endometrial cancer. Endometrial
商品
Human pancreatic cancer organoid biobank (PDAC organoids) with various KRAS mutations to aide in 3D cell culture and cancer research applications.
可生成组织和干细胞来源3D脑、胃肠道、肺和癌症肿瘤类器官模型的类器官培养产品。
Organoid culture products to generate tissue and stem cell derived 3D brain, intestinal, gut, lung and cancer tumor organoid models.
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