Nelarabine (506U78) 是一种核苷类似物 (
nucleoside analogue)，可用于 T 细胞急性淋巴细胞白血病的研究。
| 生物活性 |
Nelarabine (506U78) is anucleoside analogueand can be used for the research of T cell acute lymphoblastic leukemia (T-ALL)[1].
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体外研究
(In Vitro) |
Nelarabine (506U78) (0-20 μM; 48 h) induces cytotoxic effects in T-ALL cell lines[1].
Nelarabine (5 or 2 μM; 48 h) promotes apoptosis in sensitive T-ALL cell lines and modulates PI3K/AKT/mTOR and MEK signaling[1].
Nelarabine (10 μM; 0-48 h) resistance does not depend on expression of ENT1/2 transporters and is partly due to upregulation of PI3K, MEK, and Bcl2 signaling[1].
Cell Viability Assay[1]
| Cell Line: |
T-ALL cell lines |
| Concentration: |
0-20 μM |
| Incubation Time: |
48 h |
| Result: |
Cell viability decreased in a concentration-dependent fashion, and the IC50values ranged between 2 and 5.5 μM for sensitive cell lines (MOLT-4, HSB-2, P12, DND41, JURKAT). |
Apoptosis Analysis[1]
| Cell Line: |
MOLT-4, JURKAT, P12-ICHIKAWA and DND41 |
| Concentration: |
5 μM (2 μM for MOLT-4 cells) |
| Incubation Time: |
48 h |
| Result: |
Detected a marked increase in the percentage of early apoptotic and/or late apoptotic cells. |
Western Blot Analysis[1]
| Cell Line: |
MOLT-4, JURKAT, P12-ICHIKAWA and DND41 |
| Concentration: |
5 μM (2 μM for MOLT-4 cells) |
| Incubation Time: |
0, 6, 16, 24 and 48 h |
| Result: |
Documented a time-dependent cleavage of caspase 8, caspase 9, caspase 3, and poly(ADP-ribose) polymerase (PARP) in response to drug treatment.
Induced a marked decrease of phosphorylated AKT at Ser473, S6 ribosomal protein (S6RP) at Ser235/236, and GSK3β at Ser9. |
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体内研究
(In Vivo) |
Nelarabine (506U78) (130 mg/kg/day; i.v.; 5 days) reduces leukemic burden and extends mouse survival in NSG mice xenografted with luciferase-expressing U937 cells[2].
| Animal Model: |
NSG mice xenografted with luciferase-expressing U937 cells[2] |
| Dosage: |
130 mg/kg/day |
| Administration: |
Intravenous injection, 5 days |
| Result: |
Reduced leukemic burden and extended mouse survival. |
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| Clinical Trial |
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| 分子量 |
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| 性状 |
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| Formula |
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| CAS 号 |
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| 中文名称 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
| Powder |
-20°C |
3 years |
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4°C |
2 years |
| In solvent |
-80°C |
6 months |
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-20°C |
1 month |
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| 溶解性数据 |
In Vitro:
DMSO : 100 mg/mL(336.39 mM;Need ultrasonic)
H2O : 10 mg/mL(33.64 mM;Need ultrasonic)
配制储备液
| 1 mM |
3.3639 mL |
16.8197 mL |
33.6395 mL |
| 5 mM |
0.6728 mL |
3.3639 mL |
6.7279 mL |
| 10 mM |
0.3364 mL |
1.6820 mL |
3.3639 mL |
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请根据半岛bd体育手机客户端 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半岛bd体育手机客户端 失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。
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
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
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1.
请依序添加每种溶剂： PBS
Solubility: 5 mg/mL (16.82 mM); Clear solution; Need ultrasonic and warming and heat to 60℃
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2.
请依序添加每种溶剂： 10% DMSO40%PEG3005%Tween-8045% saline
Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.41 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
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3.
请依序添加每种溶剂： 10% DMSO90% (20%SBE-β-CDin saline)
Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.41 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
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4.
请依序添加每种溶剂： 10% DMSO90%corn oil
Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.41 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
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以上所有助溶剂都可在本网站选购。
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