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1809784-29-9

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1809784-29-9 Structure

1809784-29-9 Structure
IdentificationBack Directory
[Name]

(R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-guanidinopentanamide
[CAS]

1809784-29-9
[Synonyms]

DTP3
DTP3 inhibitor
D-Phenylalaninamide, N-acetyl-D-tyrosyl-D-arginyl-
cancer,DTP 3,inhibit,Inhibitor,Janus kinase,DNA/RNA Synthesis,NF-κB,DTP-3,tumor,GADD45β,DTP3,JAK
(R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-guanidinopentanamide
(R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-guanidinopentanamide USP/EP/BP
[Molecular Formula]

C26H35N7O5
[MDL Number]

MFCD28348368
[MOL File]

1809784-29-9.mol
[Molecular Weight]

525.6
Chemical PropertiesBack Directory
[density ]

1.35±0.1 g/cm3(Predicted)
[solubility ]

DMSO:100.0(Max Conc. mg/mL);190.26(Max Conc. mM)
Ethanol:100.0(Max Conc. mg/mL);190.26(Max Conc. mM)
Water:100.0(Max Conc. mg/mL);190.26(Max Conc. mM)
[form ]

Solid
[pka]

9.83±0.15(Predicted)
[color ]

White to off-white
[CAS DataBase Reference]

1809784-29-9
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P280-P301+P312-P302+P352-P305+P351+P338
Hazard InformationBack Directory
[Uses]

DTP3 is a selective GADD45β/MKK7 inhibitor, which inhibits the cancer-selective NF-κB survival pathway. It specifically kills cells and induces apoptosis in MM cells without being toxic to normal cells.m
[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.
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