CRT0066101

CAS: 956123-34-5 F: C18H22N6O W: 338.41

CRT0066101 is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD

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Bioactivity	CRT0066101 is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively[1]. CRT0066101 is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 has anticancer effects[2].
Invitro	CRT0066101 (5 µM; 1 h) 可阻断 Panc-1 和 Panc-28 细胞中基础和 NT 诱导的 pS916-PKD1/2（激活的 PKD1/2）。CRT0066101 消除 NT 诱导的 Hsp27 (pS82-Hsp27) 磷酸化，减弱 PKD1 介导的 NF-κB 激活，并消除 NF-κB 依赖性增殖和促生存蛋白的表达[1] .CRT0066101 显着抑制 Panc-1 细胞增殖，IC50 值为 1 µM。CRT0066101 可诱导 Panc-1 细胞凋亡 6-10 倍。CRT0066101 显着降低 Colo357、Panc-1、MiaPaCa-2 和 AsPC-1 细胞的增殖，但对 Capan-2 细胞有一定影响[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CRT0066101 相关抗体: Western Blot Analysis[1] Cell Line:
In Vivo	CRT0066101（80 mg/kg/天；口服灌胃；每天一次；持续 21 天）在 Panc-1 原位模型中可有效阻止体内肿瘤生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
CAS	956123-34-5
Formula	C18H22N6O
Molar Mass	338.41
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]. Harikumar KB, et al. A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo. Mol Cancer Ther. 2010 May;9(5):1136-46. [2]. Xi Chen, et al. Identification and assessment of new PIM2 inhibitors for treating hematologic cancers: A combined approach of energy-based virtual screening and machine learning evaluation. Arch Pharm (Weinheim). 2024 Jan 23:e2300516.

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