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364042-47-7 (A 419259)

1

Identification

A 419259 A 419259
Name A 419259
Formula C29H34N6O
MW 482.62
CAS No. 364042-47-7
EINECS
Smiles NC1=C2C(N([[email protected]]3CC[[email protected]](N4CCN(C)CC4)CC3)C=C2C5=CC=C(OC6=CC=CC=C6)C=C5)=NC=N1
Synonyms A419259;A-419259;RK 20449;RK20449;RK-20449; 7-((1r,4r)-4-(4-methylpiperazin-1-yl)cyclohexyl)-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
InChI InChI=1S/C29H34N6O/c1-33-15-17-34(18-16-33)22-9-11-23(12-10-22)35-19-26(27-28(30)31-20-32-29(27)35)21-7-13-25(14-8-21)36-24-5-3-2-4-6-24/h2-8,13-14,19-20,22-23H,9-12,15-18H2,1H3,(H2,30,31,32)/t22-,23-
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Introduction

A 419259(RK 20449) is an apoptosis inducing agent that inhibits Src family kinases (c-Src); A 419259 also induces apoptosis in CML cell ines and blocks Stat5 and Erk activation. IC50 Value: 9 nM (Src); <3 nM (Lck); <3 nM (Lyn); 3 uM (Abl) [1] Target: Src family kinase in vitro: Treatment of the Ph+ CML cell lines K-562 and Meg-01 with A-419259 resulted in growth arrest and induction of apoptosis, while the Ph- leukemia cell lines TF-1 and HEL were unaffected over the same concentration ranges.

Background Information

A 419259(RK 20449) is an apoptosis inducing agent that inhibits Src family kinases (c-Src); A 419259 also induces apoptosis in CML cell ines and blocks Stat5 and Erk activation. IC50 Value: 9 nM (Src); <3 nM (Lck); <3 nM (Lyn); 3 uM (Abl) [1] Target: Src family kinase in vitro: Treatment of the Ph+ CML cell lines K-562 and Meg-01 with A-419259 resulted in growth arrest and induction of apoptosis, while the Ph- leukemia cell lines TF-1 and HEL were unaffected over the same concentration ranges. Suppression of Ph+ cell growth by A-419259 correlated with a decrease in Src kinase autophosphorylation. A-419259 blocked Stat5 and Erk activation, consistent with the suppressive effects of the compounds on survival and proliferation [1]. A-419259 treatment blocks all Src-family kinase activity in ES cells, preventing differentiation while maintaining pluripotency. Expression of inhibitor-resistant c-Src but not c-Yes rescued the A-419259 differentiation block, resulting in a cell population with properties of both primitive ectoderm and endoderm [2]. Blockade of Src family kinases using an Src-specific tyrosine kinase inhibitor A-419259 decreased GRP-induced EGFR phosphorylation and MAPK activation in HNSCC [3]. ......by MedChemexpress Co., Ltd.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000013723

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
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Mechanism and Indication

Signaling Pathways Protein Tyrosine Kinase/RTK
Target Src
Research Area Cancer
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
A 419259 - No Development Reported
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Safety Data of A 419259

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
CHEMSCENE, LLC USA
MedChemexpress Co., Ltd. 10mg/USD180(Get quote);50mg/USD630(Get quote) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD195(Get quote);50mg/USD580(Get quote) China
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Related Products

Other Forms of 364042-47-7

Name CAS No Formula MW
A 419259 (trihydrochloride) 1435934-25-0 C29H37Cl3N6O 592.0

Recommended Compounds in Src

Name CAS No Formula MW
Scutellarein 529-53-3 C15H10O6 286.24
A 419259 (trihydrochloride) 1435934-25-0 C29H37Cl3N6O 592.0
1-Naphthyl PP1 221243-82-9 C19H19N5 317.39
XL228 898280-07-4 C22H31N9O 437.54
Dasatinib (hydrochloride) 854001-07-3 C22H27Cl2N7O2S 524.47
1-(2-Nitrovinyl)-3,4-methylenedioxybenzene 1485-00-3 C9H7NO4 193.16
PP2 172889-27-9 C15H16ClN5 301.77
PP1 172889-26-8 C16H19N5 281.36
ZM 306416 690206-97-4 C16H13ClFN3O2 333.74
AMG-47a 882663-88-9 C29H28F3N5O2 535.56
KX1-004 518058-84-9 C16H13FN2O2 284.29
AZM-475271 476159-98-5 C23H27ClN4O3 442.94
DCC-2036 1020172-07-9 C30H28FN7O3 553.59
Lck Inhibitor 847950-09-8 C31H30N8O 530.62
Lck inhibitor 2 944795-06-6 C18H17N5O2 335.36
PD173955 260415-63-2 C21H16Cl2N4OS 443.35
TG 100801 (Hydrochloride) 1018069-81-2 C33H31Cl2N5O3 616.54
TG 100801 867331-82-6 C33H30ClN5O3 580.08
TG 100572 (Hydrochloride) 867331-64-4 C26H27Cl2N5O2 512.43
TG 100572 867334-05-2 C26H26ClN5O2 475.97

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

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More Information

A 419259

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