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1809784-29-9

1809784-29-9 structure
1809784-29-9 structure
  • Name: DTP3
  • Chemical Name: DTP-3
  • CAS Number: 1809784-29-9
  • Molecular Formula: C26H35N7O5
  • Molecular Weight: 525.600
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage DNA/RNA Synthesis
  • Create Date: 2019-06-16 11:02:40
  • Modify Date: 2024-01-21 01:32:06
  • 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].

Name DTP-3
Synonyms 7UXW0T8LS8
D-Phenylalaninamide, N-acetyl-D-tyrosyl-D-arginyl-
DTP-3
N-Acetyl-D-tyrosyl-D-arginyl-D-phenylalaninamide
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].
Related Catalog
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].
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.
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.

Density 1.4±0.1 g/cm3
Molecular Formula C26H35N7O5
Molecular Weight 525.600
Exact Mass 525.269958
LogP -0.43
Appearance powder
Index of Refraction 1.637
Storage condition Store at -20°C
Water Solubility 100 mg/mL (190.26 mM)