IMR-1A | CAS#331862-41-0

IMR-1A
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406984

CAS#: 331862-41-0

Description: IMR-1A is a metabolite of IMR-1 (MedKoo Cat#: 406983). IMR-1A acts as Notch inhibitor and targeting gene transcription by disrupting Mam1 recruitment to chromatin.

Chemical Structure

IMR-1A

CAS# 331862-41-0

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406984
Name: IMR-1A
CAS#: 331862-41-0
Chemical Formula: C13H11NO5S2
Exact Mass: 325.01
Molecular Weight: 325.353
Elemental Analysis: C, 47.99; H, 3.41; N, 4.31; O, 24.59; S, 19.71

Price and Availability

Size	Price	Availability	Quantity
100mg	USD 850
200mg	USD 1250
500mg	USD 1950
1g	USD 2850
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: IMR-1A; IMR 1A; IMR1A; Inhibitor of Mastermind Recruitment-1 Acid.

IUPAC/Chemical Name: 2-[2-Methoxy-4-[(Z)-(4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene)methyl]phenoxy]acetic acid

InChi Key: DVBJNSKWHSGTDK-YHYXMXQVSA-N

InChi Code: InChI=1S/C13H11NO5S2/c1-18-9-4-7(2-3-8(9)19-6-11(15)16)5-10-12(17)14-13(20)21-10/h2-5H,6H2,1H3,(H,15,16)(H,14,17,20)/b10-5-

SMILES Code: O=C(O)COC1=CC=C(/C=C(SC(N2)=S)/C2=O)C=C1OC

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: >2 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:

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Biological target:	IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitor with an IC50 of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A.
In vitro activity:	To determine the effect of IMR-1 treatment on the assembly of the NTC in cells, Notch-dependent cell lines OE33 and 786-0 were treated with DAPT or IMR-1. Treatment of OE33 and 786-0 with IMR-1 also decreased the occupancy of Maml1 on the HES1 promoter but, in contrast to DAPT treatment, IMR-1 treatment did not affect the occupancy of Notch1 on the HES1 promoter (Fig 3A). Therefore, these data indicate that IMR-1 specifically disrupts the recruitment of Maml1 to chromatin while the binding of NICD to CSL is unaffected. Reference: Cancer Res. 2016 Jun 15;76(12):3593-603. https://pubmed.ncbi.nlm.nih.gov/27197169/
In vivo activity:	Treatment of both PDX tumors with IMR-1 significantly abrogated growth to a similar level achieved with DAPT treatment (Fig. 5A and 5B), without any significant weight loss or other visible signs of adverse effects in the treated animals (Supplementary Fig. 3). Following 24 days of treatment, tumors were harvested and Notch target gene transcription was evaluated. These data demonstrate that treatment with IMR-1 dramatically reduced the expression level of the tested Notch target genes (Hes1, HeyL, and Notch3; Fig. 5C) in both PDX models. Reference: Cancer Res. 2016 Jun 15;76(12):3593-603. https://pubmed.ncbi.nlm.nih.gov/27197169/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	4.0	12.29
	Water	1.0	3.07

Preparing Stock Solutions

The following data is based on the product molecular weight 325.35 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. Astudillo L, Da Silva TG, Wang Z, Han X, Jin K, VanWye J, Zhu X, Weaver K, Oashi T, Lopes PE, Orton D, Neitzel LR, Lee E, Landgraf R, Robbins DJ, MacKerell AD Jr, Capobianco AJ. The Small Molecule IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis. Cancer Res. 2016 Jun 15;76(12):3593-603. doi: 10.1158/0008-5472.CAN-16-0061. Epub 2016 Apr 13. PMID: 27197169; PMCID: PMC4911243.
In vitro protocol:	1. Astudillo L, Da Silva TG, Wang Z, Han X, Jin K, VanWye J, Zhu X, Weaver K, Oashi T, Lopes PE, Orton D, Neitzel LR, Lee E, Landgraf R, Robbins DJ, MacKerell AD Jr, Capobianco AJ. The Small Molecule IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis. Cancer Res. 2016 Jun 15;76(12):3593-603. doi: 10.1158/0008-5472.CAN-16-0061. Epub 2016 Apr 13. PMID: 27197169; PMCID: PMC4911243.
In vivo protocol:	1. Astudillo L, Da Silva TG, Wang Z, Han X, Jin K, VanWye J, Zhu X, Weaver K, Oashi T, Lopes PE, Orton D, Neitzel LR, Lee E, Landgraf R, Robbins DJ, MacKerell AD Jr, Capobianco AJ. The Small Molecule IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis. Cancer Res. 2016 Jun 15;76(12):3593-603. doi: 10.1158/0008-5472.CAN-16-0061. Epub 2016 Apr 13. PMID: 27197169; PMCID: PMC4911243.

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9: Hager M, Mikuz G, Haufe H, Kolbitsch C, Moser KB, Moser PL. Association between atherosclerosis and urothelial tumors of the renal pelvis. World J Urol. 2008 Aug;26(4):375-9. doi: 10.1007/s00345-008-0271-2. PubMed PMID: 18483813.

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11: Lewycka S, Mwansambo C, Rosato M, Kazembe P, Phiri T, Mganga A, Chapota H, Malamba F, Kainja E, Newell ML, Greco G, Pulkki-Brännström AM, Skordis-Worrall J, Vergnano S, Osrin D, Costello A. Effect of women's groups and volunteer peer counselling on rates of mortality, morbidity, and health behaviours in mothers and children in rural Malawi (MaiMwana): a factorial, cluster-randomised controlled trial. Lancet. 2013 May 18;381(9879):1721-35. doi: 10.1016/S0140-6736(12)61959-X. PubMed PMID: 23683639; PubMed Central PMCID: PMC3796349.

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