[CAS NO. 324759-76-4] CCT020312

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PRODUCTS SPECIFICATIONS [324759-76-4]

Catalog

HY-119240

Brand

MCE

CAS

324759-76-4

DESCRIPTION [324759-76-4]

Overview

MDL	-
Molecular Weight	650.40
Molecular Formula	C31H30Br2N4O2
SMILES	O=C1NC2=C(C(C3=CC=CC=C3)=C1C4=NN(C(C4)C5=CC=C(C=C5)Br)C(CCN(CC)CC)=O)C=C(C=C2)Br

For research use only. We do not sell to patients.

11 Publications Citing Use of MCE

Summary

CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.

IC50 & Target

EIF2AK3/PERK ^[1] ^[2] .

In Vitro

Treatment of HT29 cells with CCT020312 for 24 hours reveals a concentration-dependent loss of P-S608-pRB signal, with a linear response between 1.8 and 6.1 μM ^[1] .
CCT020312 treatment effectively inhibits cell proliferation (as measured at 96 hours) even if treatment is for 2 hours only with subsequent compound washout, indicating that CCT020312 is capable of eliciting durable rather than transient cytostasis ^[1] .
Treatment of HT29 cells with 10 μM CCT020312 for 24 hours reduces the amount of the G1/S cyclins D1, D2, E and A as well as the CDK catalytic subunit CDK2 and increased the level of the CDK inhibitor p27KIP1 present in such cells ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Treatment of 15-week-old wildtype mice with the PERK activator CCT020312 (1-5 mg/kg; i.p.; once daily for 3 days) leads to increased levels of phosphorylated PERK and NRF2 in brain homogenates ^[2] .
P301S transgenic mice treated with CCT020312 (2 mg/kg; i.p.; once daily for 6 weeks) performes significantly better in Morris water maze ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	9-week-old P301S tau transgenic mice ^[2]
Dosage:	2 mg/kg
Administration:	Intraperitoneal injection; once daily for 6 weeks
Result:	P301S transgenic mice treated with CCT020312 performed significantly better in Morris water maze.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 153.75 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5375 mL	7.6876 mL	15.3752 mL
5 mM	0.3075 mL	1.5375 mL	3.0750 mL
10 mM	0.1538 mL	0.7688 mL	1.5375 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (3.20 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 2.08 mg/mL (3.20 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.20 mM); Clear solution

* All of the co-solvents are available by MCE.