MT1 | BET inhibitor | CAS#2060573-82-0

MedKoo Cat#: 407972 | Name: MT1 BET inhibitor

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Description:

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

MT1, also known as (Bis-CPI203)-PEG7, is a highly potent BET bromodomain inhibitor. MT1 is an intramolecular bivalent BRD4 binder that is more than 100-fold more potent, in cellular assays, than the corresponding monovalent antagonist, JQ1. MT1 significantly (P < 0.05) delayed leukemia progression in mice, as compared to JQ1.

Chemical Structure

MT1 BET inhibitor

CAS#2060573-82-0

Theoretical Analysis

MedKoo Cat#: 407972

Name: MT1 BET inhibitor

CAS#: 2060573-82-0

Chemical Formula: C54H66Cl2N10O9S2

Exact Mass: 1132.3833

Molecular Weight: 1134.20

Elemental Analysis: C, 57.19; H, 5.87; Cl, 6.25; N, 12.35; O, 12.70; S, 5.65

Price and Availability

Size	Price	Availability	Quantity
1mg	USD 450.00	2 Weeks

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Synonym

MT1; MT-1; MT 1; Bis-CPI203-PEG7; Bis-CPI-203-PEG7; (Bis-CPI203)-PEG7;

IUPAC/Chemical Name

N,N'-(3,6,9,12,15,18,21-heptaoxatricosane-1,23-diyl)bis(2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide)

InChi Key

JNSLBXJNVHYNNW-CXNSMIOJSA-N

InChi Code

InChI=1S/C54H66Cl2N10O9S2/c1-33-35(3)76-53-47(33)49(39-7-11-41(55)12-8-39)59-43(51-63-61-37(5)65(51)53)31-45(67)57-15-17-69-19-21-71-23-25-73-27-29-75-30-28-74-26-24-72-22-20-70-18-16-58-46(68)32-44-52-64-62-38(6)66(52)54-48(34(2)36(4)77-54)50(60-44)40-9-13-42(56)14-10-40/h7-14,43-44H,15-32H2,1-6H3,(H,57,67)(H,58,68)/t43-,44-/m0/s1

SMILES Code

O=C(NCCOCCOCCOCCOCCOCCOCCOCCNC(C[C@@H](C1=NN=C(N21)C)N=C(C3=C2SC(C)=C3C)C4=CC=C(C=C4)Cl)=O)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5

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:

MT1 is a bivalent chemical probe of BET bromodomains, with an IC50 of 0.789 nM for BRD4(1).

In vitro activity:

Significant apoptosis was observed by caspase-3 and PARP cleavage after treatment with MT1 (Fig. 5b). These cellular events followed after HEXIM1 upregulation and MYC downregulation. Early and late apoptosis were assessed with annexin-V and propidium iodide staining to compare apoptosis induction between MT1 and JQ1 (Fig. 5c and Supplementary Fig. 12). Importantly, MT1 induced a greater degree of apoptosis at 10-fold lower concentrations than JQ1. Reference: Nat Chem Biol. 2016 Dec;12(12):1089-1096. https://pubmed.ncbi.nlm.nih.gov/27775715/

In vivo activity:

To determine whether MT1 could attenuate the growth of BRD4-dependent leukemia as a single agent in vivo, this study selected an aggressive disseminated leukemia model (mCherry+, Luciferase+, MV4;11) and treated animals with established disease using equimolar (44.2 µmol/kg) and half an equivalent (22.1 µmol/kg) of MT1 compared to JQ1 for 14 days. During the study, leukemic burden was monitored by non-invasive bioluminescence imaging. Even half an equivalent of MT1 significantly reduced leukemic burden over the course of the study compared to either vehicle or JQ1 (Fig. 6a). Post-mortem analysis of leukemic burden in bone marrow by FACS also revealed significantly decreased mCherry+ disease with MT1 administration at 22.1 µg/kg (Fig. 6b). Reference: Nat Chem Biol. 2016 Dec;12(12):1089-1096. https://pubmed.ncbi.nlm.nih.gov/27775715/

	Solvent	mg/mL	mM
Solubility
	DMSO	150.0	132.25

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 1,134.20 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:

Tanaka M, Roberts JM, Seo HS, Souza A, Paulk J, Scott TG, DeAngelo SL, Dhe-Paganon S, Bradner JE. Design and characterization of bivalent BET inhibitors. Nat Chem Biol. 2016 Dec;12(12):1089-1096. doi: 10.1038/nchembio.2209. Epub 2016 Oct 24. PMID: 27775715; PMCID: PMC5117811.

In vitro protocol:

In vivo protocol:

1: Tanaka M, Roberts JM, Seo HS, Souza A, Paulk J, Scott TG, DeAngelo SL, Dhe-Paganon S, Bradner JE. Design and characterization of bivalent BET inhibitors. Nat Chem Biol. 2016 Dec;12(12):1089-1096. doi: 10.1038/nchembio.2209. Epub 2016 Oct 24. PubMed PMID: 27775715; PubMed Central PMCID: PMC5117811.

Description:

Chemical Structure

Theoretical Analysis

Price and Availability

Preparing Stock Solutions

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