[CAS NO. ] Syk-IN-4

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PRODUCTS SPECIFICATIONS

Catalog

HY-131341

Brand

MCE

CAS

-

DESCRIPTION

Overview

MDL	-
Molecular Weight	419.48
Molecular Formula	C21H25N9O
SMILES	CC1=NN(C=C1CN(C)C)C2=NC(NC3=CC=C(N(C)N=C4C(NC)=O)C4=C3)=NC=C2

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

Summary

Syk-IN-4 is a potent, selective and orally bioavailable SYK inhibitor with an IC ₅₀ of 0.31 nM. SYK has emerged as a potential target for autoimmunity and hematological cancers ^[1] .

IC50 & Target

IC50: 0.31 nM (SYK) ^[1]

In Vitro

Syk-IN-4 is a potent inhibitor of hERG with an IC ₅₀ of 3.0 μM ^[1] .
Syk-IN-4 inhibits SUDHL-4 and T cell proliferation with GI ₅₀ s of 0.24 and 2.6 µM, respectively ^[1] .

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

In Vivo

Syk-IN-4 exhibits moderate oral bioavailability (60%) following oral administration (1 mg/kg) in male Hans Wistar rats ^[1] .
Syk-IN-4 exhibits high plasma clearance (151 mL/min/kg) combined with large volumes of distribution (1.0 L/kg respectively) following i.v. administration (0.5 mg/kg) in male Hans Wistar rats ^[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 : 62.5 mg/mL ( 148.99 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3839 mL	11.9195 mL	23.8390 mL
5 mM	0.4768 mL	2.3839 mL	4.7678 mL
10 mM	0.2384 mL	1.1920 mL	2.3839 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: ≥ 2.08 mg/mL (4.96 mM); Clear solution
2.

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

Solubility: 2.08 mg/mL (4.96 mM); Suspended solution; Need ultrasonic
3.

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

Solubility: ≥ 2.08 mg/mL (4.96 mM); Clear solution

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

References

[1] Neil P Grimster, et al. Optimization of a Series of Potent, Selective and Orally Bioavailable SYK Inhibitors. Bioorg Med Chem Lett. 2020 Jul 24;127433.