CCT020312 | CAS# 324759-76-4 | EIF2AK3 Activator

CCT020312
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407383

CAS#: 324759-76-4

Description: CCT020312 is a potent and selective EIF2AK3 Activator. CCT020312 modulates the biological activity of EIF2AK3. CCT020312 sensitizes cancer cells with defective taxane-induced EIF2A phosphorylation to paclitaxel treatment. CCT020312 is a novel small molecule chemical tool for the selective activation of EIF2A-mediated translation control with utility for proof-of-concept applications in EIF2A-centered therapeutic approaches, and as a chemical starting point for pathway selective agent development. CCT020312 is potent, and EIF2AK3 selective agent and can act as a sensitizer to chemotherapy-associated stresses as elicited by taxanes.

Chemical Structure

CCT020312

CAS# 324759-76-4

Instruction

Theoretical Analysis

MedKoo Cat#: 407383
Name: CCT020312
CAS#: 324759-76-4
Chemical Formula: C31H30Br2N4O2
Exact Mass: 648.07
Molecular Weight: 650.415
Elemental Analysis: C, 57.25; H, 4.65; Br, 24.57; N, 8.61; O, 4.92

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 350	2 Weeks
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: CCT020312; CCT-020312; CCT 020312.

IUPAC/Chemical Name: 6-Bromo-3-[5-(4-bromo-phenyl)-1-(3-diethylamino-propionyl)-4,5-dihydro-1H-pyrazol-3-yl]-4-phenyl-1H-quinolin-2-one

InChi Key: OAXDKXMGESZLKV-UHFFFAOYSA-N

InChi Code: InChI=1S/C31H30Br2N4O2/c1-3-36(4-2)17-16-28(38)37-27(20-10-12-22(32)13-11-20)19-26(35-37)30-29(21-8-6-5-7-9-21)24-18-23(33)14-15-25(24)34-31(30)39/h5-15,18,27H,3-4,16-17,19H2,1-2H3,(H,34,39)

SMILES Code: O=C1NC2=C(C=C(Br)C=C2)C(C3=CC=CC=C3)=C1C4=NN(C(CCN(CC)CC)=O)C(C5=CC=C(Br)C=C5)C4

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: Human cancers often contain genetic alterations that disable G1/S checkpoint control and loss of this checkpoint is thought to critically contribute to cancer generation by permitting inappropriate proliferation and distorting fate-driven cell cycle exit. The identification of cell permeable small molecules that activate the G1/S checkpoint may therefore represent a broadly applicable and clinically effective strategy for the treatment of cancer

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 650.42 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:
In vitro protocol:
In vivo protocol:

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1: Stockwell SR, Platt G, Barrie SE, Zoumpoulidou G, Te Poele RH, Aherne GW,
Wilson SC, Sheldrake P, McDonald E, Venet M, Soudy C, Elustondo F, Rigoreau L,
Blagg J, Workman P, Garrett MD, Mittnacht S. Mechanism-based screen for G1/S
checkpoint activators identifies a selective activator of EIF2AK3/PERK
signalling. PLoS One. 2012;7(1):e28568. doi: 10.1371/journal.pone.0028568. PubMed
PMID: 22253692; PubMed Central PMCID: PMC3257223.

2: Bruch J, Xu H, Rösler TW, De Andrade A, Kuhn PH, Lichtenthaler SF, Arzberger
T, Winklhofer KF, Müller U, Höglinger GU. PERK activation mitigates tau pathology
in vitro and in vivo. EMBO Mol Med. 2017 Feb 1. pii: e201606664. doi:
10.15252/emmm.201606664. [Epub ahead of print] PubMed PMID: 28148553.

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CCT020312 featured