[CAS NO. 1003311-62-3] c-Kit-IN-5-1

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PRODUCTS SPECIFICATIONS [1003311-62-3]

Catalog

HY-18302

Brand

MCE

CAS

1003311-62-3

DESCRIPTION [1003311-62-3]

Overview

MDL	-
Molecular Weight	395.41
Molecular Formula	C23H17N5O2
SMILES	O=C1C(C2=CC3=CN=C(N)N=C3C=C2)=C(C)C=CN1C4=CC=C(C5=NC=CO5)C=C4

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

Summary

c-Kit-IN-5 is potent inhibitor of c-Kit , with IC ₅₀ s of 22 nM and 16 nM in kinase assay and cell assay, respectively. c-Kit-IN-5 shows more than 200-fold selectivity for c-Kit over KDR, p38, Lck, and Src . c-Kit-IN-5 also exhibits desirable pharmacokinetic properties ^[1] .

In Vitro

c-Kit-IN-5 (compound 25) shows more than 200-fold selectivity against KDR, p38, Lck, and Src (IC ₅₀ =>5.0, 40, 7.8 , and >5.0 μM, respectively) ^[1] .

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

In Vivo

c-Kit-IN-5 (compound 25) (1 mg/kg; i.v.) exhibits CL (0.46 L/h/kg) and V _dss (1.59 L/kg) in rats ^[1] .
c-Kit-IN-5 (10 mg/kg; p.o.) exhibits AUC _0-t (9860 ng•h/mL) C _max (1230 ng/mL), T _1/2 (2.6 h), and F (39%) in rats ^[1] .

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 : 25 mg/mL ( 63.23 mM ; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5290 mL	12.6451 mL	25.2902 mL
5 mM	0.5058 mL	2.5290 mL	5.0580 mL
10 mM	0.2529 mL	1.2645 mL	2.5290 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: 1.67 mg/mL (4.22 mM); Suspended solution; Need ultrasonic
2.

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

Solubility: 1.67 mg/mL (4.22 mM); Suspended solution; Need ultrasonic

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

References

[1] Hu E, et, al. Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit. J Med Chem. 2008 Jun 12;51(11):3065-8.