dTAGV-1 TFA|cas:2624313-15-9|西域试剂

dTAGV-1 TFA,99.92%

产品编号：Bellancom-145514| CAS NO：2624313-15-9| 分子式：C₇₀H₉₁F₃N₆O₁₆S| 分子量：1361.56

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-145514		￥6800.00	杭州北京（现货）
Bellancom-145514		￥11500.00	杭州北京（现货）

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dTAGV-1 TFA

产品介绍

dTAGV-1 TFA 是一种有效和选择性的突变 FKBP12^F36V 融合蛋白降解剂。dTAGV-1 TFA 可以在体内诱导 FKBP12^F36V-Nluc 降解。

生物活性

dTAGV-1 TFA is a potent and selective degrader of mutant FKBP12^F36V fusion proteins. dTAGV-1 TFA can induce degradation of FKBP12^F36V-Nluc in vivo.

体外研究

dTAGV-1 (0.1 nM-10 μM; 24 h) TFA induces potent degradation of FKBP12^F36V-Nluc with no effects on FKBP12^WT-Nluc in 293FT cells.
dTAGV-1 (125-2000 nM; 24 h) TFA co-treatment with THAL-SNS-032 leads to pronounced degradation of both LACZ-FKBP12^F36V and CDK9.
dTAGV-1 (500 nM; 1-24 h) TFA leads to rapid KRAS^G12V and pERK1/2 degradation.
dTAGV-1 (50-5000 nM; 24 h) TFA enables EWS/FLI degradation in Ewing sarcoma.

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

体内研究

dTAGV-1 (35 mg/kg; i.p. once daily for 4 days) TFA induces degradation of FKBP12^F36V-Nluc in mice.
dTAGV-1 (2-10 mg/kg; i.p.) TFA exhbits half-lives (T_1/2=3.64 and 4.4 h), C_max (595 and 2123 ng/mL) and great exposure (AUC_inf =3136 and 18517 h•ng/mL) in mice.
dTAGV-1 (2 mg/kg; i.v.) TFA exhbits half-life (T_1/2=3.02 h), C_max (7780 ng/mL) and great exposure (AUC_inf =3329 h•ng/mL) in mice.

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

Animal Model:	8-week-old immunocompromised female mice were transplanted with MV4;11 luc-FKBP12^F36V cells
Dosage:	35 mg/kg
Administration:	I.p. once daily for 4 days
Result:	Observed striking loss of bioluminescent signal 4 h after the first and three administrations. Degradation evident 28 h after the final administration.

体内研究

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

Animal Model:	8-week-old immunocompromised female mice were transplanted with MV4;11 luc-FKBP12^F36V cells
Dosage:	35 mg/kg
Administration:	I.p. once daily for 4 days
Result:	Observed striking loss of bioluminescent signal 4 h after the first and three administrations. Degradation evident 28 h after the final administration.

性状

Solid

溶解性数据

In Vitro:

DMSO : 37.5 mg/mL (27.54 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.7345 mL	3.6723 mL	7.3445 mL
5 mM	0.1469 mL	0.7345 mL	1.4689 mL
10 mM	0.0734 mL	0.3672 mL	0.7345 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 (sealed storage, away from moisture and light)。-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: ≥ 3.75 mg/mL (2.75 mM); Clear solution

此方案可获得 ≥ 3.75 mg/mL (2.75 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 37.5 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% corn oil
Solubility: ≥ 3.75 mg/mL (2.75 mM); Clear solution

此方案可获得 ≥ 3.75 mg/mL (2.75 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 37.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。