[CAS NO. 1435934-25-0]  A419259trihydrochloride

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PRODUCTS SPECIFICATIONS [1435934-25-0]

Distributor
Catalog
AS939218
Brand
Arctom Scientific
CAS
1435934-25-0

DESCRIPTION [1435934-25-0]

Overview

MDL-
Molecular Weight592.00
Molecular FormulaC29H37Cl3N6O
SMILESNC1=C2C(N([C@H]3CC[C@H](N4CCN(C)CC4)CC3)C=C2C5=CC=C(OC6=CC=CC=C6)C=C5)=NC=N1.[H]Cl.[H]Cl.[H]Cl

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


Summary

A 419259 trihydrochloride is a Src family kinases inhibitor with IC 50 s of 9 nM, 3 nM and 3 nM for Src , Lck and Lyn , respectively.


IC50 & Target

IC50: 9 nM (Src), <3 nM (Lck), <3 nM (Lyn), 3 μM (Abl) [1]


In Vitro

A 419259 Trihydrochloride is a second-generation pyrrolo-pyrimidine designed to enhance selectivity towards the Src family relative to other cytoplasmic tyrosine kinases. A-419259 inhibits K-562 cells with an IC 50 between 0.1 and 0.3 μM, and Meg-01 proliferation with an IC 50 of approximately 0.1 μM. A-419259 also potently induces apoptosis in K-562 cells beginning at 0.1 μM and increasing in a dose-dependent manner. PP2 inhibits Src kinase autophosphorylation in both Ph + cell lines (K-562 and Meg-01) with an IC 50 between 3 and 10 μM, while A-419259 blocks kinase activation between 0.1 and 0.3 μM. A-419259 strongly inhibits DAGM/Bcr-Abl cell proliferation in the absence of IL-3 with an IC 50 between 0.1 and 0.3 μM [1] . A-419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, and blocks proliferation and induces apoptosis in CML cell lines. A-419259 inhibits overall SFK activity in K562 and other CML cell lines with an IC 50 value of 0.1-0.3 μM [2] .

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

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)


Solvent & Solubility

In Vitro:

H 2 O : ≥ 55 mg/mL ( 92.91 mM )

DMSO : 1 mg/mL ( 1.69 mM ; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6892 mL 8.4459 mL 16.8919 mL
5 mM 0.3378 mL 1.6892 mL 3.3784 mL
10 mM 0.1689 mL 0.8446 mL 1.6892 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: PBS

    Solubility: 100 mg/mL (168.92 mM); Clear solution; Need ultrasonic

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