LP-922761 | CAS#1454808-95-7 | AAK1 inhibitor

MedKoo Cat#: 561294 | Name: LP-922761

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

LP-922761 is a potent and selective AAK1 inhibitor with an in vitro IC50 value of 4.8 ± 0.8 nM and a cellular IC50 value of 7.6 ± 0.7 nM.

Chemical Structure

LP-922761

CAS#1454808-95-7

Theoretical Analysis

MedKoo Cat#: 561294

Name: LP-922761

CAS#: 1454808-95-7

Chemical Formula: C21H26N6O3

Exact Mass: 410.2066

Molecular Weight: 410.48

Elemental Analysis: C, 61.45; H, 6.38; N, 20.47; O, 11.69

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 465.00	2 Weeks

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Related CAS #

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Synonym

LP-922761; LP922761; LP 922761;

IUPAC/Chemical Name

(2-[3-(4-Carbamoyl-phenyl)imidazo[1,2-b]pyridazin-6-ylamino]ethyl)methylcarbamic acid tert-butyl ester

InChi Key

YNQNYIHMAZLJAV-UHFFFAOYSA-N

InChi Code

InChI=1S/C21H26N6O3/c1-21(2,3)30-20(29)26(4)12-11-23-17-9-10-18-24-13-16(27(18)25-17)14-5-7-15(8-6-14)19(22)28/h5-10,13H,11-12H2,1-4H3,(H2,22,28)(H,23,25)

SMILES Code

O=C(OC(C)(C)C)N(CCNC1=NN2C(C=C1)=NC=C2C3=CC=C(C(N)=O)C=C3)C

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AA K1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively.

In vitro activity:

LP-922761 is a potent and selective AAK1 inhibitor with an in vitro IC50 value of 4.8 ± 0.8 nM and a cellular IC50 value of 7.6 ± 0.7 nM (Table 1). Reference: J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. https://pubmed.ncbi.nlm.nih.gov/27411717/

In vivo activity:

TBD

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	20.5	49.99

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 410.48 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Kostich W, Hamman BD, Li YW, Naidu S, Dandapani K, Feng J, Easton A, Bourin C, Baker K, Allen J, Savelieva K, Louis JV, Dokania M, Elavazhagan S, Vattikundala P, Sharma V, Das ML, Shankar G, Kumar A, Holenarsipur VK, Gulianello M, Molski T, Brown JM, Lewis M, Huang Y, Lu Y, Pieschl R, O'Malley K, Lippy J, Nouraldeen A, Lanthorn TH, Ye G, Wilson A, Balakrishnan A, Denton R, Grace JE, Lentz KA, Santone KS, Bi Y, Main A, Swaffield J, Carson K, Mandlekar S, Vikramadithyan RK, Nara SJ, Dzierba C, Bronson J, Macor JE, Zaczek R, Westphal R, Kiss L, Bristow L, Conway CM, Zambrowicz B, Albright CF. Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain. J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. doi: 10.1124/jpet.116.235333. Epub 2016 Jul 13. PMID: 27411717; PMCID: PMC4998676.

In vitro protocol:

In vivo protocol:

TBD

1: Kostich W, Hamman BD, Li Y-W, et al. Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain. The Journal of Pharmacology and Experimental Therapeutics. 2016;358(3):371-386. doi:10.1124/jpet.116.235333.