(E)-Daporinad (Synonyms: 达珀利奈; FK866; APO866) 纯度: 99.94%
(E)-Daporinad (FK866) 是烟酰胺磷酸核糖转移酶 (NMPRTase; Nampt) 的有效抑制剂, IC50 为 0.09 nM。
(E)-Daporinad Chemical Structure
CAS No. : 658084-64-1
规格 | 价格 | 是否有货 | 数量 |
---|---|---|---|
Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥729 | In-stock | |
5 mg | ¥663 | In-stock | |
10 mg | ¥1252 | In-stock | |
50 mg | ¥4201 | In-stock | |
100 mg | ¥6800 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
(E)-Daporinad 相关产品
•相关化合物库:
- Covalent Screening Library Plus
- Drug Repurposing Compound Library Plus
- Clinical Compound Library Plus
- Bioactive Compound Library Plus
- Metabolism/Protease Compound Library
- Anti-Cancer Compound Library
- Clinical Compound Library
- Autophagy Compound Library
- Drug Repurposing Compound Library
- Covalent Screening Library
生物活性 |
(E)-Daporinad (FK866) is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with an IC50 of 0.09 nM. |
IC50 & Target |
IC50: 0.09 nM (NMPRTase) |
||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
体外研究 (In Vitro) |
Nampt inhibition with (E)-Daporinad (FK866) induces significant NAD+ intracellular reduction and selectively kills MM cells. (E)-Daporinad (FK866)-induced cell death is associated with inhibition of Nampt activity, rather than protein expression, and higher NAD+ baseline levels in MM cells than normal PBMCs confer (E)-Daporinad (FK866) sensitivity. (E)-Daporinad (FK866) abrogates the survival advantage conferred by the bone marrow microenvironment[1]. (E)-Daporinad (FK866) prevents the [Ca2+]i increase induced by different mitogens and reduces the Ca2+ content of TG-responsive Ca2+ stores in Jurkat and in activated PBLs. (E)-Daporinad (FK866) reduces the Ca2+ content of TG-responsive Ca2+ stores in Jurkat cells but not in Bcl2-Jurkat cells[2]. Inhibition of NAMPT by (E)-Daporinad (FK866), or inhibition of SIRT by nicotinamide decreases proliferation and triggered death of 293T cells involving the p53 acetylation pathway[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
体内研究 (In Vivo) |
(E)-Daporinad (FK866) (30 mg/kg, i.p.) decreases the tumor burden in CB17-SCID mice, and the tumor tissue demonstrates a significant decrease in ERK phosphorylation and proteolytic cleavage of LC3[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
Clinical Trial |
|
||||||||||||||||
分子量 |
391.51 |
||||||||||||||||
Formula |
C24H29N3O2 |
||||||||||||||||
CAS 号 |
658084-64-1 |
||||||||||||||||
中文名称 |
达珀利奈 |
||||||||||||||||
运输条件 |
Room temperature in continental US; may vary elsewhere. |
||||||||||||||||
储存方式 |
|
||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : ≥ 50 mg/mL (127.71 mM) H2O : 1 mg/mL (2.55 mM; Need ultrasonic) * “≥” means soluble, but saturation unknown. 配制储备液
*
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
|
||||||||||||||||
参考文献 |
|
Cell Assay [1] |
MM1S cells (2×104 cells/well) are cultured for 72 and 96 hours in BMSC-coated 96-well plates in the presence or absence of drug. DNA synthesis is measured by (3H)-thymidine uptake, with (3H)-thymidine added (0.5 μCi/well) during the last 8 hours of cultures. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
---|---|
Animal Administration [1] |
CB17-SCID mice (28-35 days old) are irradiated (200 cGy), and then inoculated subcutaneously in the right flank with 3×106 MM1S cells in 100 μL RPMI 1640. After detection of tumor (2 weeks after the injection), 7 mice are treated intraperitoneally with either vehicle or (E)-Daporinad (FK866) (30 mg/kg body weight) twice a day for 4 days, repeated weekly over 3 weeks. Caliper measurements of the longest perpendicular tumor diameters are performed twice a week to estimate the tumor volume using the following formula: length×width2×0.5. Tumor growth inhibition (TGI) is calculated. Animals are killed when tumors reach 2 cm3 or the mice appear moribund. Survival is evaluated from the first day of treatment until death. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
|