[CAS NO. 1233339-22-4] AZ20

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PRODUCTS SPECIFICATIONS [1233339-22-4]

Catalog

HY-15557

Brand

MCE

CAS

1233339-22-4

DESCRIPTION [1233339-22-4]

Overview

MDL	MFCD25976730
Molecular Weight	412.51
Molecular Formula	C21H24N4O3S
SMILES	O=S(C1(C2=CC(N3[C@H](C)COCC3)=NC(C4=CC=CC5=C4C=CN5)=N2)CC1)(C)=O

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

10 Publications Citing Use of MCE

Summary

AZ20 is a potent and selective inhibitor of ATR with an IC ₅₀ of 5 nM, and has 8-fold selectivity against mTOR (IC ₅₀ =38 nM).

IC50 & Target

ATR

5 nM (IC ₅₀ )

mTOR

38 nM (IC ₅₀ )

PI3Kα

13000 nM (IC ₅₀ )

In Vitro

AZ20 inhibits ATR immunoprecipitated from HeLa nuclear extracts with an IC ₅₀ of 5 nM and ATR mediated phosphorylation of Chk1 in HT29 colorectal adenocarcinoma tumor cells with an IC ₅₀ of 50 nM ^[1] .

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

In Vivo

AZ20 (25, 50 mg/kg, p.o.) has high permeability combined with good stability to rat hepatocytes and, despite the lack of progress in achieving markedly higher solubility, has respectable bioavailability in a low dose rat PK study. AZ20 (25, 50 mg/kg, p.o.) leads to significant tumor growth inhibition in female nude mice bearing LoVo tumors ^[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 : ≥ 100 mg/mL ( 242.42 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4242 mL	12.1209 mL	24.2418 mL
5 mM	0.4848 mL	2.4242 mL	4.8484 mL
10 mM	0.2424 mL	1.2121 mL	2.4242 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 (6.06 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution

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

References

[1] Foote KM, et al. Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. J Med Chem. 2013 Mar 14