[CAS NO. 1448671-31-5] AZD3965

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PRODUCTS SPECIFICATIONS [1448671-31-5]

Catalog

HY-12750

Brand

MCE

CAS

1448671-31-5

DESCRIPTION [1448671-31-5]

Overview

MDL	MFCD28963899
Molecular Weight	515.51
Molecular Formula	C21H24F3N5O5S
SMILES	O=C1N(C(C)C)C2=C(C(C(N3OC[C@@](C)(O)C3)=O)=C(CC4=C(C)NN=C4C(F)(F)F)S2)C(N1C)=O

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

30 Publications Citing Use of MCE

Summary

AZD3965 is a selective MCT1 inhibitor with a K _i of 1.6 nM, showing 6-fold selectivity over MCT2.

IC50 & Target

Ki: 1.6 nM (MCT1) ^[1]

In Vitro

AZD3965 is designed to selectively inhibit Monocarboxylate transporter-1 (MCT1) and will therefore be expected to influence the movement of lactate into and out of cells ^[1] . AZD3965 treatment causes a 3.7 fold increase in intracellular lactate in hypoxic COR-L103 and 3.7 fold and 3.9 fold increases in normoxic and hypoxic NCI-H1048 cells respectively. In all other cases a <1.9 fold increase is observed. These data are consistent with AZD3965 blocking lactate transport in cells where AZD3965 also reduces cell number and is consistent with AZD3965 acting via inhibition of MCT1. When MCT1 is overexpressed the EC ₅₀ of NCI-H1048 is increased from 0.14 nM to 10.5 nM in NCI-H1048 cells. This is consistent with AZD3965 acting via MCT1 inhibition ^[2] .

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

In Vivo

COR-L103 tumor bearing mice are treated with 100 mg/kg AZD3965 or vehicle BIDfor 21 days and the tumor volume monitored. Pharmacokinetic analysis demonstrates that 100 mg/kg AZD3965 BID results in concentrations of free AZD3965 predicted to inhibit lactate transport. AZD3965 treatment significantly reduces the growth of COR-L103 tumors, although tumor regression is not seen, consistent with AZD3965 only targeting the hypoxic fraction of the tumor ^[2] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01791595	Cancer Research UK\|AstraZeneca	Adult Solid Tumor\|Diffuse Large B Cell Lymphoma\|Burkitt Lymphoma	April 23, 2013	Phase 1

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 ( 193.98 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9398 mL	9.6991 mL	19.3983 mL
5 mM	0.3880 mL	1.9398 mL	3.8797 mL
10 mM	0.1940 mL	0.9699 mL	1.9398 mL

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

In Vivo:

1.

Add each solvent one by one: 0.5% HPMC >> 0.2%Tween80

Solubility: 5 mg/mL (9.70 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 20% HP-β-CD in saline

Solubility: 5 mg/mL (9.70 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C
3.

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

Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution
4.

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

Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution
5.

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

Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

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