| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
GADD45β/MKK7
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| ln Vitro |
DTP3 (10 μM; 1-21 days) causes the development of phosphorylated JNK to appear as early as 24 hours after the strong and tumor-specific induction of JNK activation and apoptosis[2].
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| ln Vivo |
DTP3 TFA (sc; 14.5 mg/kg/day; 28 days) essentially eliminates established subcutaneous myeloma xenografts in mice and has demonstrated a remarkable tumor shrinkage[2]. The t1/2, CL, and Vd values of DTP3 TFA (intravenous injection; 10 mg/kg/day) are 1.26 hours, 27.13 ML/min/kg, and 2.80 L/kg, respectively[2].
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: Multiple myeloma (MM) cell lines Tested Concentrations: 10 μM Incubation Duration: 1, 3, 5, 14, 21 days Experimental Results: Caused the appearance of phosphorylated JNK, as early as 24 hrs (hours). |
| Animal Protocol |
Animal/Disease Models: 6 to 8-week old male NOD/SCID (severe combined immunodeficient) mouse (NOD.CB17-Prkdcscid/IcrCrl; Charles River)[2]
Doses: 14.5 mg/kg Route of Administration: Sc; daily; 28 days Experimental Results: Had shown a dramatic shrinkage of the tumors. Animal/Disease Models: CD1 male mice of 25-30 g[2] Doses: 10 mg/kg (pharmacokinetic/PK Study) Route of Administration: intravenous (iv)injection Experimental Results: Had t1/2 of 1.26 hrs (hours), CL of 27.13 ML/min/kg, and Vd of 2.80 L/kg. |
| References |
[1]. Tornatore L, et al. Preclinical toxicology and safety pharmacology of the first-in-class GADD45β/MKK7inhibitor and clinical candidate, DTP3. Toxicol Rep. 2019 Apr 19;6:369-379.
[2]. Tornatore L, et al. Cancer-selective targeting of the NF-κB survival pathway with GADD45β/MKK7 inhibitors. Cancer Cell. 2014 Oct 13;26(4):495-508. |
| Molecular Formula |
C28H36F3N7O7
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|---|---|
| Molecular Weight |
639.62
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| Exact Mass |
639.26
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| CAS # |
2759216-46-9
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| Related CAS # |
DTP3;1809784-29-9
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| Appearance |
Powder
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| SMILES |
CC(=O)N[C@H](CC1=CC=C(C=C1)O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CC2=CC=CC=C2)C(=O)N.C(=O)(C(F)(F)F)O
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| InChi Key |
JCVMRDQSOXBZIO-AFYLVLOISA-N
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| InChi Code |
InChI=1S/C26H35N7O5.C2HF3O2/c1-16(34)31-22(15-18-9-11-19(35)12-10-18)25(38)32-20(8-5-13-30-26(28)29)24(37)33-21(23(27)36)14-17-6-3-2-4-7-17;3-2(4,5)1(6)7/h2-4,6-7,9-12,20-22,35H,5,8,13-15H2,1H3,(H2,27,36)(H,31,34)(H,32,38)(H,33,37)(H4,28,29,30);(H,6,7)/t20-,21-,22-;/m1./s1
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| Chemical Name |
(2R)-2-[[(2R)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-N-[(2R)-1-amino-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)pentanamide;2,2,2-trifluoroacetic acid
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| Synonyms |
DTP3 TFA
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~156.3 mM)
DMSO : ~50 mg/mL (~78.2 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (156.34 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5634 mL | 7.8171 mL | 15.6343 mL | |
| 5 mM | 0.3127 mL | 1.5634 mL | 3.1269 mL | |
| 10 mM | 0.1563 mL | 0.7817 mL | 1.5634 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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