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DTP3

  Cat. No.:  DC7849   Featured
Chemical Structure
1809784-29-9
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Field of application
For the detailed information of DTP3, the solubility of DTP3 in water, the solubility of DTP3 in DMSO, the solubility of DTP3 in PBS buffer, the animal experiment (test) of DTP3, the cell expriment (test) of DTP3, the in vivo, in vitro and clinical trial test of DTP3, the EC50, IC50,and affinity,of DTP3, Please contact DC Chemicals..
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1809784-29-9
Chemical Name: (R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-((diaminomethylene)amino)pentanamide
Synonyms: DTP3; DTP-3; DTP 3;
SMILES: O=C(N[C@H](CC1=CC=CC=C1)C(N)=O)[C@H](NC([C@H](NC(C)=O)CC2=CC=C(O)C=C2)=O)CCC/N=C(N)\N
Formula: C26H35N7O5
M.Wt: 525.61
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: DTP3 TFA is a potent and selective GADD45β/MKK7 inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway[1].
In Vivo: DTP3 TFA (s.c.; 14.5 mg/kg/day; 28 days) has shown a dramatic shrinkage of the tumors, and virtually eradicates established subcutaneous myeloma xenografts in mice[2]. DTP3 TFA (intravenous injection; 10 mg/kg/day) has t1/2 of 1.26 hours, CL of 27.13 ML/min/kg, and Vd of 2.80 L/kg[2]. Animal Model: 6 to 8-week old male NOD/SCID mice (NOD.CB17-Prkdcscid/IcrCrl; Charles River)[2] Dosage: 14.5 mg/kg Administration: S.c.; daily; 28 days Result: Had shown a dramatic shrinkage of the tumors. Animal Model: CD1 male mice of 25-30 g[2] Dosage: 10 mg/kg (Pharmacokinetic Study) Administration: Intravenous injection Result: Had t1/2 of 1.26 hours, CL of 27.13 ML/min/kg, and Vd of 2.80 L/kg.
In Vitro: DTP3 (10 μM; 1-21 days) causes the potent and tumor-selective induction of JNK activation and apoptosis, as shown by the appearance of phosphorylated JNK, as early as 24 hours[2].
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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