MedKoo Cat#: 555974 | Name: DTP3 inhibitor
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

DTP3 is a selective GADD45β/MKK7 inhibitor, which inhibits cancer-selective NF-κB survival pathway. DTP3 specifically kills MM cells, ex vivo and in vivo, ablating MM xenografts in mice, with no apparent adverse effects, nor evident toxicity to healthy cells. DTP3 combines on-target-selective pharmacology, therapeutic anticancer efficacy, favourable drug-like properties, long plasma half-life and good bioavailability, with no target-organs of toxicity and no adverse effects preclusive of its clinical development in oncology, upon daily repeat-dose administration in both rodent and non-rodent species.

Chemical Structure

DTP3 inhibitor
DTP3 inhibitor
CAS# 1809784-29-9

Theoretical Analysis

MedKoo Cat#: 555974

Name: DTP3 inhibitor

CAS#: 1809784-29-9

Chemical Formula: C26H35N7O5

Exact Mass: 525.2700

Molecular Weight: 525.61

Elemental Analysis: C, 59.41; H, 6.71; N, 18.65; O, 15.22

Price and Availability

Size Price Availability Quantity
50mg USD 550.00 2 Weeks
100mg USD 950.00 2 Weeks
200mg USD 1,450.00 2 Weeks
500mg USD 2,450.00 2 Weeks
1g USD 3,250.00 2 Weeks
2g USD 5,450.00 2 Weeks
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Related CAS #
No Data
Synonym
DTP3; DTP-3; DTP 3; NSC785669; NSC 785669; NSC-785669
IUPAC/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
InChi Key
AOUZPXZGMZUQQS-YPAWHYETSA-N
InChi Code
InChI=1S/C26H35N7O5/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/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)/t20-,21-,22-/m1/s1
SMILES Code
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
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Biological target:
DTP3 is a potent and selective GADD45β/MKK7 inhibitor.
In vitro activity:
DTP3 has similar anticancer potency to the clinical standard, bortezomib, but more than 100-fold higher cancer cell specificity in vitro. Reference: Cancer Cell. 2014 Oct 13;26(4):495-508. https://pubmed.ncbi.nlm.nih.gov/25314077/
In vivo activity:
As a result, DTP3 specifically kills MM cells, ex vivo and in vivo, ablating MM xenografts in mice, with no apparent adverse effects, nor evident toxicity to healthy cells. Reference: Toxicol Rep. 2019 Apr 19;6:369-379. https://pubmed.ncbi.nlm.nih.gov/31080744/
Solvent mg/mL mM
Solubility
DMSO 100.0 190.26
Ethanol 100.0 190.26
Water 100.0 190.26
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 525.61 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Tornatore L, Capece D, D'Andrea D, Begalli F, Verzella D, Bennett J, Acton G, Campbell EA, Kelly J, Tarbit M, Adams N, Bannoo S, Leonardi A, Sandomenico A, Raimondo D, Ruvo M, Chambery A, Oblak M, Al-Obaidi MJ, Kaczmarski RS, Gabriel I, Oakervee HE, Kaiser MF, Wechalekar A, Benjamin R, Apperley JF, Auner HW, Franzoso G. Preclinical toxicology and safety pharmacology of the first-in-class GADD45β/MKK7 inhibitor and clinical candidate, DTP3. Toxicol Rep. 2019 Apr 19;6:369-379. doi: 10.1016/j.toxrep.2019.04.006. PMID: 31080744; PMCID: PMC6502747. 2. Tornatore L, Sandomenico A, Raimondo D, Low C, Rocci A, Tralau-Stewart C, Capece D, D'Andrea D, Bua M, Boyle E, van Duin M, Zoppoli P, Jaxa-Chamiec A, Thotakura AK, Dyson J, Walker BA, Leonardi A, Chambery A, Driessen C, Sonneveld P, Morgan G, Palumbo A, Tramontano A, Rahemtulla A, Ruvo M, Franzoso G. Cancer-selective targeting of the NF-κB survival pathway with GADD45β/MKK7 inhibitors. Cancer Cell. 2014 Oct 13;26(4):495-508. doi: 10.1016/j.ccr.2014.07.027. Erratum in: Cancer Cell. 2014 Dec 8;26(6):938. PMID: 25314077; PMCID: PMC4197335.
In vitro protocol:
1. Tornatore L, Sandomenico A, Raimondo D, Low C, Rocci A, Tralau-Stewart C, Capece D, D'Andrea D, Bua M, Boyle E, van Duin M, Zoppoli P, Jaxa-Chamiec A, Thotakura AK, Dyson J, Walker BA, Leonardi A, Chambery A, Driessen C, Sonneveld P, Morgan G, Palumbo A, Tramontano A, Rahemtulla A, Ruvo M, Franzoso G. Cancer-selective targeting of the NF-κB survival pathway with GADD45β/MKK7 inhibitors. Cancer Cell. 2014 Oct 13;26(4):495-508. doi: 10.1016/j.ccr.2014.07.027. Erratum in: Cancer Cell. 2014 Dec 8;26(6):938. PMID: 25314077; PMCID: PMC4197335.
In vivo protocol:
1. Tornatore L, Capece D, D'Andrea D, Begalli F, Verzella D, Bennett J, Acton G, Campbell EA, Kelly J, Tarbit M, Adams N, Bannoo S, Leonardi A, Sandomenico A, Raimondo D, Ruvo M, Chambery A, Oblak M, Al-Obaidi MJ, Kaczmarski RS, Gabriel I, Oakervee HE, Kaiser MF, Wechalekar A, Benjamin R, Apperley JF, Auner HW, Franzoso G. Preclinical toxicology and safety pharmacology of the first-in-class GADD45β/MKK7 inhibitor and clinical candidate, DTP3. Toxicol Rep. 2019 Apr 19;6:369-379. doi: 10.1016/j.toxrep.2019.04.006. PMID: 31080744; PMCID: PMC6502747.
Tornatore L, Capece D, D'Andrea D, Begalli F, Verzella D, Bennett J, Acton G, Campbell EA, Kelly J, Tarbit M, Adams N, Bannoo S, Leonardi A, Sandomenico A, Raimondo D, Ruvo M, Chambery A, Oblak M, Al-Obaidi MJ, Kaczmarski RS, Gabriel I, Oakervee HE, Kaiser MF, Wechalekar A, Benjamin R, Apperley JF, Auner HW, Franzoso G. Preclinical toxicology and safety pharmacology of the first-in-class GADD45β/MKK7 inhibitor and clinical candidate, DTP3. Toxicol Rep. 2019 Apr 19;6:369-379. doi: 10.1016/j.toxrep.2019.04.006. PMID: 31080744; PMCID: PMC6502747.