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Chemical Structure| 1435934-25-0 Chemical Structure| 1435934-25-0

Structure of A 419259 3HCl
CAS No.: 1435934-25-0

Chemical Structure| 1435934-25-0

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A 419259 3HCl is a broad-spectrum pyrrolo-pyrimidine inhibitor, designed to enhance selectivity towards the Src family with IC50 of 9 nM, < 3 nM and < 3 nM for Src, Lck and Lyn, respectively.

Synonyms: RK 20449 trihydrochloride; A 419259 trihydrochloride; A-419259 trihydrochloride, A-419259 3HCl

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Product Details of A 419259 3HCl

CAS No. :1435934-25-0
Formula : C29H37Cl3N6O
M.W : 592.00
SMILES Code : NC1=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
Synonyms :
RK 20449 trihydrochloride; A 419259 trihydrochloride; A-419259 trihydrochloride, A-419259 3HCl
MDL No. :MFCD19690922

Safety of A 419259 3HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of A 419259 3HCl

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
293T cells 100 nM and 1000 nM To determine the effect each mutation on HCK sensitivity to A-419259 PMC8136437
Rat-2 fibroblasts 1 μM two weeks Selection of cell colonies resistant to A-419259 PMC8136437
TF-1/Bcr-Abl cells 0.1-1.0 μM 5 h To evaluate the inhibitory effect of A-419259 on Hck activity. Results showed that wild-type Hck was partially inhibited at 0.1 and 0.3 μM and completely blocked at 1 μM. The Hck-T338M mutant showed significant resistance, with partial inhibition observed only at 1 μM. PMC2738638
K562 cells 0.1-1.0 μM 5 h To evaluate the inhibitory effect of A-419259 on Hck activity. Results showed that A-419259 partially inhibited wild-type Hck at 0.1 μM and completely inhibited it at 0.3 and 1.0 μM. The Hck-T338M mutant exhibited significant resistance at the same concentrations. PMC2738638
Rat2 fibroblasts 1 μM To validate the function of c-Yes inhibitor-resistant mutants, results showed that A-419259 treatment inhibits wild-type c-Yes activity but has no effect on the c-Yes-IR mutant. PMC3875617
Mouse ES cells 1 μM 48 h To test the effect of A-419259 on ES cell differentiation, results showed that A-419259 treatment blocks all Src-family kinase activity in ES cells, preventing differentiation while maintaining pluripotency. PMC3875617

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.69mL

0.34mL

0.17mL

8.45mL

1.69mL

0.84mL

16.89mL

3.38mL

1.69mL

Dissolving Methods
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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