ALK5-IN-79_product_DataBase

Bioactivity	ALK5-IN-79 (compound 57) is an ALK inhibitor with anticancer activity, by blocking TGF-β1/SMAD signaling pathway. ALK5-IN-79 attenuates the production of extracellular matrix (ECM) and deposition of collagen. ALK5-IN-79 exhibits adequate pharmacokinetic (PK) properties and good in vivo tolerance.
Invitro	ALK5-IN-79 (1000 nM； 2 小时) 对 ALK5，SRC， LCK， BRAF (V600E)， ET， PDGFRα， EGFR 和 KDR 具有强至中度的抑制活性(抑制率大于20%)[1]。ALK5-IN-79 (0，0.125，0.25，0.5，1.0 and 2.0 μM；1 小时) 抑制 smad3 的磷酸化且呈剂量依赖性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> ALK5-IN-79 相关抗体: Western Blot Analysis[1] Cell Line:
In Vivo	ALK5-IN-79 (300 mg/kg，每天腹腔注射连续 7 天) 没有使小鼠体重明显下降，具有体内深入研究安全性[1]。ALK5-IN-79 (10 mg/kg 和 50 mg/kg 每隔一天静脉注射连续 24 天) 使用后肿瘤生长抑制率分别为 61.9% 和 80.5% 在 Syngeneic 模型中，ALK5-IN-79 (10 mg/kg 和 50 mg/kg 每隔一天筋脉注射连续 24 天) 使用后肿瘤生长抑制率分别为 62.1% 和 75.6% 在 PANC-1 皮下异种移植模型中。ALK5-IN-79 以剂量依赖的方式抑制胰腺癌肿瘤的生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
CAS	2725056-38-0
Formula	C23H27N7O
Molar Mass	417.51
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Yubo Wang et al. Design, synthesis and evaluation of a pyrazolo[3,4-d]pyrimidine derivative as a novel and potent TGFβ1R1 inhibitor. European Journal of Medicinal Chemistry. Volume 271, 5 May 2024, 116395

PeptideDB

ALK5-IN-79

CAS: 2725056-38-0 F: C23H27N7O W: 417.51