dTRIM 24 | CAS#2170695-14-2 | protein degrader

MedKoo Cat#: 584783 | Name: dTRIM 24

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Description:

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

dTRIM 24 is a TRIM24 degrading PROTAC.

Chemical Structure

dTRIM 24

CAS#2170695-14-2

Theoretical Analysis

MedKoo Cat#: 584783

Name: dTRIM 24

CAS#: 2170695-14-2

Chemical Formula: C55H68N8O13S2

Exact Mass: 1112.4347

Molecular Weight: 1113.31

Elemental Analysis: C, 59.34; H, 6.16; N, 10.07; O, 18.68; S, 5.76

Price and Availability

Size	Price	Availability	Quantity
1mg	USD 350.00	2 Weeks
5mg	USD 750.00	2 Weeks

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Synonym

dTRIM 24; dTRIM24; dTRIM-24

IUPAC/Chemical Name

(2S,4R)-1-((S)-15-(tert-Butyl)-1-(3-(N-(1,3-dimethyl-2-oxo-6-(3-propoxyphenoxy)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)sulfamoyl)phenyl)-1,13-dioxo-5,8,11-trioxa-2,14-diazahexadecan-16-oyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

InChi Key

QUQTXFIMYFMULC-OGOZKGDESA-N

InChi Code

InChI=1S/C55H68N8O13S2/c1-8-20-75-40-12-10-13-41(28-40)76-47-30-45-44(61(6)54(69)62(45)7)29-43(47)60-78(70,71)42-14-9-11-38(26-42)51(66)56-19-21-72-22-23-73-24-25-74-33-48(65)59-50(55(3,4)5)53(68)63-32-39(64)27-46(63)52(67)57-31-36-15-17-37(18-16-36)49-35(2)58-34-77-49/h9-18,26,28-30,34,39,46,50,60,64H,8,19-25,27,31-33H2,1-7H3,(H,56,66)(H,57,67)(H,59,65)/t39-,46+,50-/m1/s1

SMILES Code

O=C([C@H]1N(C([C@H](C(C)(C)C)NC(COCCOCCOCCNC(C2=CC=CC(S(=O)(NC3=C(OC4=CC=CC(OCCC)=C4)C=C(C(N5C)=C3)N(C)C5=O)=O)=C2)=O)=O)=O)C[C@H](O)C1)NCC6=CC=C(C7=C(C)N=CS7)C=C6

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

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

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

Product Data

Instruction

View handling instruction

Biological target:

dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24.

In vitro activity:

This study therefore performed a series of experiments, aiming to verify whether specific TRIM24 inhibition suppresses GBM malignant functions using dTRIM24 and IACS-9571, two novel selective TRIM24 antagonists. These data showed that TRIM24 inhibitors serve as effective agents for inhibiting cell propagation and invasion of several patient-derived GBM stem cells (GSCs), and these effects are mediated partially through suppression of the TRIM24-SOX2 axis. Reference: J Transl Med. 2021 Dec 9;19(1):505. https://pubmed.ncbi.nlm.nih.gov/34886858/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	61.1	54.96
	Ethanol	22.3	20.02

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 1,113.31 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.

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. Han M, Sun Y. Pharmacological targeting of Tripartite Motif Containing 24 for the treatment of glioblastoma. J Transl Med. 2021 Dec 9;19(1):505. doi: 10.1186/s12967-021-03158-w. PMID: 34886858; PMCID: PMC8662887. 2. Gechijian LN, Buckley DL, Lawlor MA, Reyes JM, Paulk J, Ott CJ, Winter GE, Erb MA, Scott TG, Xu M, Seo HS, Dhe-Paganon S, Kwiatkowski NP, Perry JA, Qi J, Gray NS, Bradner JE. Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nat Chem Biol. 2018 Apr;14(4):405-412. doi: 10.1038/s41589-018-0010-y. Epub 2018 Mar 5. PMID: 29507391; PMCID: PMC5866761.

In vitro protocol:

In vivo protocol:

TBD

Gechijian et al (2018) Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nat.Chem.Biol. 14 405 PMID: 29507391