上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
CRT0066101 dihydrochloride 纯度: 99.53%
CRT0066101 dihydrochloride是有效,选择性的 PKD 抑制剂,对PKD1,2和3的IC50值分别为1,2.5和2 nM。
CRT0066101 dihydrochloride Chemical Structure
CAS No. : 1883545-60-5
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥902 | In-stock | |
5 mg | ¥820 | In-stock | |
10 mg | ¥1500 | In-stock | |
25 mg | ¥3400 | In-stock | |
50 mg | ¥6100 | In-stock | |
100 mg | 询价 | ||
200 mg | 询价 |
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CRT0066101 dihydrochloride 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Apoptosis Compound Library
- Kinase Inhibitor Library
- Anti-Cancer Compound Library
- Targeted Diversity Library
生物活性 |
CRT0066101 dihydrochloride is a potent and specific PKD inhibitor with IC50 values of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
CRT0066101 specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple cancer cell types including A549 (lung) and MiaPaCa-2 (pancreas). CRT0066101 significantly inhibits Panc-1 cell proliferation with an IC50 value of 1 µM. Treatment with CRT0066101 results in a 6-10 fold induction of apoptosis in Panc-1 cells. CRT0066101 significantly reduces cell proliferation of Colo357, Panc-1, MiaPaCa-2, and AsPC-1 cells but has a modest effect in Capan-2 cells. CRT0066101 (5 µM) blocks both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2) in Panc-1 and Panc-28 cells. CRT0066101 reduces PKD-dependent NF-κB activation and NF-κB-dependent gene expressions in Panc-1[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Optimal therapeutic concentrations (8 µM) of CRT0066101 are detectable 6 h after oral administration of this drug. CRT0066101 given orally (80 mg/kg/day) for 28 days significantly abrogates PaCa growth in Panc-1 subcutaneous xenograft model. Activated PKD1/2 expression in the treated tumor-explants is significantly inhibited with peak tumor concentration (12 µM) of CRT0066101 achieved within 2 h after oral administration. Further, CRT0066101 given orally (80 mg/kg/day) for 21 days in Panc-1 orthotopic model potently blocks tumor growth in vivo. CRT0066101 significantly reduces Ki-67+ proliferation index, increases TUNEL+ apoptotic cells (p<0.05), and abrogates expression of NF-κB-dependent proteins including cyclin D1, survivin, and cIAP-1[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
411.33 |
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Formula |
C18H24Cl2N6O |
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CAS 号 |
1883545-60-5 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
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溶解性数据 |
In Vitro:
H2O : 50 mg/mL (121.56 mM; Need ultrasonic) DMSO : ≥ 25 mg/mL (60.78 mM) * “≥” means soluble, but saturation unknown. 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Animal Administration [1] |
Mice: Nineteen days after implantation of Panc-1 cells, tumor areas are, on average 0.3 cm2 and are randomized into the following groups (n=8 mice per group): (a) vehicle (control) 5% dextrose administered by oral gavage once daily and (b) 80 mg/kg CRT0066101 dissolved in 5% dextrose administered by oral gavage once daily. Tumors are measured in 2 dimensions every 2 to 3 days by calipers and area is calculated by multiplying length by width. Therapy is given until tumors reached their designated size limits (1.44 cm2) or until day 24 in CRT0066101 treated group. Final tumor areas are compared among groups using a Student’s t test and Fisher’s exact test with p<0.05[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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参考文献 |
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