[CAS NO. 1353552-97-2] Poseltinib

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PRODUCTS SPECIFICATIONS [1353552-97-2]

Catalog

HY-109010

Brand

MCE

CAS

1353552-97-2

DESCRIPTION [1353552-97-2]

Overview

MDL	MFCD31729279
Molecular Weight	470.52
Molecular Formula	C26H26N6O3
SMILES	O=C(C=C)NC1=CC=CC(OC2=C(OC=C3)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1

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

Summary

Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor ( IC ₅₀ =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK , and reveales potent inhibition of B cell receptor ( BCR ), Fc receptor ( FcR ), Toll-like receptor ( TLR ) mediated signaling ^[1] .

IC50 & Target

TLRs

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03099148	Eli Lilly and Company	Healthy	April 4, 2017	Phase 1
NCT03083561	Eli Lilly and Company	Healthy	March 15, 2017	Phase 1
NCT01765478	Hanmi Pharmaceutical Company Limited	Rheumatoid Arthritis	January 2013	Phase 1
NCT02628028	Eli Lilly and Company	Rheumatoid Arthritis	August 22, 2016	Phase 2

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 ( 212.53 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1253 mL	10.6265 mL	21.2531 mL
5 mM	0.4251 mL	2.1253 mL	4.2506 mL
10 mM	0.2125 mL	1.0627 mL	2.1253 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: ≥ 7.5 mg/mL (15.94 mM); Clear solution
2.

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

Solubility: ≥ 7.5 mg/mL (15.94 mM); Clear solution

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

References

[1] Kim YY, et al. HM71224, a selective Bruton's tyrosine kinase inhibitor, attenuates the development of murine lupus. Arthritis Res Ther. 2017 Sep 26;19(1):211.

Synonyms

2-Propenamide, N-[3-[[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]furo[3,2-d]pyrimidin-4-yl]oxy]phenyl]-

N-[3-[[2-[[4-(4-Methyl-1-piperazinyl)phenyl]amino]furo[3,2-d]pyrimidin-4-yl]oxy]phenyl]-2-propenamide

Poseltinib

HM 71224

LY 3337641