TL02-59|cas:1315330-17-6|西域试剂

TL02-59,99.84%

产品编号：Bellancom-112852| CAS NO：1315330-17-6| 分子式：C₃₂H₃₄F₃N₅O₄| 分子量：609.64

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货号	价格	库存与货期
Bellancom-112852	￥2800.00	杭州北京（现货）
Bellancom-112852	￥4500.00	杭州北京（现货）
Bellancom-112852	￥14000.00	杭州北京（现货）

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TL02-59

产品介绍

TL02-59 是一种具有口服活性，选择性的 Src-家族激酶 Fgr 抑制剂，IC₅₀ 为 0.03 nM。TL02-59 抑制 Src-家族激酶 Lyn 和 Hck，IC₅₀ 分别为 0.1 nM 和 160 nM。TL02-59 有效抑制急性髓性白血病 (AML) 细胞生长。

生物活性

TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC₅₀ of 0.03 nM. TL02-59 inhibits Lyn and Hck with IC₅₀s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth.

体外研究

TL02-59 (0.1-1000 nM; 6 hours) potently inhibits Fgr autophosphorylation in TF-1 cells, with paritial inhibition at 0.1-1 nM and complete inhibition above 10 nM. Hck, Lyn and Flt3 are inhibited in the 100 to 1000 nM range.
TL02-59 inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency.
TL02-59 induces growth arrest in primary AML bone marrow samples.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	TF-1 myeloid cells
Concentration:	0.1, 1, 10, 100, 1000 nM
Incubation Time:	6 hours
Result:	Inhibited Fgr autophosphorylation in TF-1 cells.

体内研究
(In Vivo)

TL02-59 (oral administration; 1 and 10 mg/kg; for three weeks) completely eliminates AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement.
TL02-59 has a t_1/2 of 5.7 h by i.v injection and 6.5 h by p.o. administration, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NOD.Cg-Prkdc^scidIl2rg^tm1Wjl/SzJ (NSG) mice with human MV4-11 AML cells
Dosage:	1 and 10 mg/kg
Administration:	Oral; for three weeks
Result:	Eliminated AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NOD.Cg-Prkdc^scidIl2rg^tm1Wjl/SzJ (NSG) mice with human MV4-11 AML cells
Dosage:	1 and 10 mg/kg
Administration:	Oral; for three weeks
Result:	Eliminated AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NOD.Cg-Prkdc^scidIl2rg^tm1Wjl/SzJ (NSG) mice with human MV4-11 AML cells
Dosage:	1 and 10 mg/kg
Administration:	Oral; for three weeks
Result:	Eliminated AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (205.04 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6403 mL	8.2016 mL	16.4031 mL
5 mM	0.3281 mL	1.6403 mL	3.2806 mL
10 mM	0.1640 mL	0.8202 mL	1.6403 mL

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.41 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.41 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.41 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。