[CAS NO. 1338934-59-0] MKC8866

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PRODUCTS SPECIFICATIONS [1338934-59-0]

Catalog

HY-104040

Brand

MCE

CAS

1338934-59-0

DESCRIPTION [1338934-59-0]

Overview

MDL	MFCD31540824
Molecular Weight	361.35
Molecular Formula	C18H19NO7
SMILES	O=CC1=C(O2)C(C(C)=C(CC(N3CCOCC3)=O)C2=O)=CC(OC)=C1O

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

8 Publications Citing Use of MCE

Summary

MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC ₅₀ of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC ₅₀ of 0.52 μM and unstresses RPMI 8226 cells with an IC ₅₀ of 0.14 μM ^[1] . MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth ^[2] .

IC50 & Target

IC50: 0.29 μM (IRE1 RNase) ^[1]

In Vitro

MKC8866 (20 μM; 6 days) decreases proliferation of all breast cancer cell lines ^[2] .
MKC8866 (20 μM; 48 hours) reduces the number of cells entering S phase ^[2] .
MKC8866 (0.2-10 μM; 3 days) suppresses the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells ^[1] .
MKC8866 (20 μM; 72 hours) is sufficient to completely block NSC 125973-induced expression of XBP1s ^[1] .

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

Cell Proliferation Assay ^[2]

Cell Line:	MCF7, SKBR3, MDA-MB-231 and MCF10A cells
Concentration:	20 μM
Incubation Time:	For 6 days
Result:	Decreased proliferation of all breast cancer cell lines.

Cell Cycle Analysis ^[2]

Cell Line:	MDA-MB-231, MCF7 and SKBR3 cells
Concentration:	20 μM
Incubation Time:	48 hours
Result:	Reduced the number of cells entering S phase.

Cell Cycle Analysis ^[1]

Cell Line:	LNCaP, VCaP, 22Rv1 and C4-2B cells
Concentration:	0.2, 0.5, 1, 5, 10 μM
Incubation Time:	3 days
Result:	Suppressed the viability of all four cell lines in a dose-dependent manner.

Cell Cycle Analysis ^[2]

Cell Line:	MDA-MB-231 cells
Concentration:	20 μM
Incubation Time:	72 hours
Result:	Completely blocked NSC 125973-induced expression of XBP1s.

In Vivo

MKC8866 (oral ; 300 mg/kg; for 28 days) reduces tumor regrowth post-NSC 125973 withdrawal ^[1] .

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

Animal Model:	Female athymic nude mice with MDA-MB-231 tumor ^[1]
Dosage:	300 mg/kg
Administration:	Oral; for 28 days
Result:	Reduced tumor regrowth post-NSC 125973 withdrawal.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 16.67 mg/mL ( 46.13 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7674 mL	13.8370 mL	27.6740 mL
5 mM	0.5535 mL	2.7674 mL	5.5348 mL
10 mM	0.2767 mL	1.3837 mL	2.7674 mL

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

In Vivo:

1.

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

Solubility: ≥ 6.75 mg/mL (18.68 mM); Clear solution
2.

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

Solubility: ≥ 1.67 mg/mL (4.62 mM); Clear solution
3.

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

Solubility: ≥ 1.67 mg/mL (4.62 mM); Clear solution

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