[CAS NO. 1333377-65-3] CHR-6494

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1333377-65-3]

Catalog

HY-15217

Brand

MCE

CAS

1333377-65-3

DESCRIPTION [1333377-65-3]

Overview

MDL	MFCD22666352
Molecular Weight	292.34
Molecular Formula	C16H16N6
SMILES	CCCNC(C=C1)=NN2C1=NC=C2C3=CC(C=NN4)=C4C=C3

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

4 Publications Citing Use of MCE

Summary

CHR-6494 is a potent inhibitor of haspin , with an IC ₅₀ of 2 nM. CHR-6494 inhibits histone H3T3 phosphorylation. CHR-6494 can be used in the research of cancer ^[1] .

IC50 & Target

haspin

2 nM (IC ₅₀ )

In Vitro

CHR-6494 (0-10 ^-5 nM; 72 hours) dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cells, with IC ₅₀ s of 500 nM, 473 nM, 752 nM and 1059 nM, respectively ^[1] .
CHR-6494 (500 nM) produces a mitotic catastrophe with abnormal morphology of the mitotic spindle and centrosome amplification, and upregulates the spindle assembly checkpoint protein BUB1 and the marker of mitotic arrest cyclin B1 ^[1] .
CHR-6494 exhibits inhibitory activities against melanoma cell lines, including BRAFV600E mutants, NRAS mutants, and wild type cells, with IC ₅₀ s ranging from 396 nM to 1229 nM ^[2] .
CHR-6494 (300 nM and 600 nM; 72 hours) induces apoptosis, increases caspase 3/7 activity by 3- and 6-fold, respectively in COLO-792 cells, and to 8.5- and 16-fold in RPMI-7951 cells ^[2] .
CHR-6494 in combination with MEK inhibitors synergistically inhibits viability of melanoma cells, enhances apoptosis in melanoma cells, modulates cell cycle progression independently by arresting melanoma cells at different phases, and suppresses migration of melanoma cells ^[2] .
CHR-6494 (50, 200 nM; 1 week) enhances the antiproliferative effects of MLN8237 in MDA-MB-231, SKBR3 breast cancer cells ^[3] .
CHR-6494 (200 nM; 72 hours) enhances the apoptosis of MDA-MB-231 and SKBR3 cells when combined with MLN8237 ^[3] .

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

In Vivo

CHR-6494 (50 mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumor and cuases no obvious body weight change in nude mice bearing HCT-116 human colorectal cancer cells ^[1] .
CHR-6494 (20 mg/kg; intraperitoneal injection for 15 consecutive days) inhibits the tumor volume and weight compared with the control group in nude mice bearing MDA-MB-231 xenograft tumors ^[3] .
CHR-6494 (20 mg/kg; intraperitoneal injection for 15 consecutive days) enhances the tumor volume and weight inhibition of MLN8237 (20 mg/kg; p.o.) in vivo ^[3] .

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

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 : 50 mg/mL ( 171.03 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.4207 mL	17.1034 mL	34.2067 mL
5 mM	0.6841 mL	3.4207 mL	6.8413 mL
10 mM	0.3421 mL	1.7103 mL	3.4207 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: ≥ 2.5 mg/mL (8.55 mM); Clear solution
2.

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

Solubility: 1 mg/mL (3.42 mM); Suspended solution; Need ultrasonic

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