| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| ln Vitro |
dTAGV-1 (0.1 nM-10 μM; 24 h) induced potent degradation of FKBP12F36V-Nluc, but had no effect on FKBP12WT-Nluc in 293FT cells[1]. Co-treatment with dTAGV-1 (125-2000 nM; 24 h) with THAL-SNS-032 resulted in significant degradation of both LACZ-FKBP12F36V and CDK9[1]. dTAGV-1 (500 nM; 1-24 h) caused rapid degradation of KRASG12V and pERK1/2[1]. dTAGV-1 (50-5000 nM; 24 h) promoted the degradation of EWS/FLI in Ewing's sarcoma[1].
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|---|---|
| ln Vivo |
dTAGV-1 (35 mg/kg; intraperitoneal injection, once daily for 4 days) can induce the degradation of FKBP12F36V-Nluc in mice[1]. dTAGV-1 (2-10 mg/kg; intraperitoneal injection) showed a half-life (T1/2 = 3.64 and 4.4 h), Cmax (595 and 2123 ng/mL) and high exposure (AUCinf = 3136 and 18517 h ng/mL) in the model[1]. dTAGV-1 (2 mg/kg; intravenous injection) showed a half-life (T1/2 = 3.02 h), Cmax (7780 ng/mL) and high exposure in mice (AUCinf = 3329 h ng/mL)[1].
|
| Animal Protocol |
Animal/Disease Models: 8-week-old immunocompromised female mice were transplanted with MV4;11 luc-FKBP12F36V cells[1]
Doses: 35 mg/kg Route of Administration: Intraperitoneal injection (i.p.); once daily for 3 days Experimental Results: Significantly reduced the bioluminescent signal 4 h after the first administration. The signal continuously decreased 4 h after each of the three administrations, and degradation was still evident 28 h after the final administration. |
| References |
| Molecular Formula |
C68H90N6O14S
|
|---|---|
| Molecular Weight |
1247.54
|
| CAS # |
2451573-86-5
|
| Related CAS # |
dTAGV-1 TFA; dTAGV-1 hydrochloride; 2624313-16-0
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~75 mg/mL (~60.12 mM; with sonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.75 mg/mL (3.01 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one)),clear solution.
For example, if 1 mL of working solution is to be prepared, you can Add 100 μL of 37.5 mg/mL clarified DMSO stock solution to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8016 mL | 4.0079 mL | 8.0158 mL | |
| 5 mM | 0.1603 mL | 0.8016 mL | 1.6032 mL | |
| 10 mM | 0.0802 mL | 0.4008 mL | 0.8016 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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