[CAS NO. 1620574-24-4] DLK-IN-1

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PRODUCTS SPECIFICATIONS [1620574-24-4]

Catalog

HY-114331

Brand

MCE

CAS

1620574-24-4

DESCRIPTION [1620574-24-4]

Overview

MDL	MFCD31813737
Molecular Weight	423.43
Molecular Formula	C20H24F3N5O2
SMILES	CC(N1C([C@@H]2[C@]3([H])[C@@]2([H])CN(C4COC4)C3)=CC(C5=CN=C(N)C(OC(F)(F)F)=C5)=N1)C

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

Summary

DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12) , with a K _i of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer’s Disease.

IC50 & Target

Ki: 3 nM (DLK) ^[1] .

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL ( 147.60 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3617 mL	11.8083 mL	23.6167 mL
5 mM	0.4723 mL	2.3617 mL	4.7233 mL
10 mM	0.2362 mL	1.1808 mL	2.3617 mL

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

In Vivo:

1.

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

Solubility: ≥ 2.08 mg/mL (4.91 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (4.91 mM); Clear solution

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

References

[1] Patel S, et al. Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease. J Med Chem. 2017 Oct 12;60(19):8083-8102.