ChemicalBook > CAS DataBase List > A 419259 trihydrochloride

A 419259 trihydrochloride

Product Name
A 419259 trihydrochloride
CAS No.
364042-47-7
Chemical Name
A 419259 trihydrochloride
Synonyms
RK20449;A419259;RK-20449;A 419259;RK 20449;A-419259;A-419259 HCl;A 419259 trihydrochloride;7-((1r,4r)-4-(4-methylpiperazin-1-yl)cyclohexyl)-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine;7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]-5-(4-phenoxyphenyl)-
CBNumber
CB12535657
Molecular Formula
C29H34N6O
Formula Weight
482.62
MOL File
364042-47-7.mol
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A 419259 trihydrochloride Property

Boiling point:
686.4±55.0 °C(Predicted)
Density 
1.29±0.1 g/cm3(Predicted)
storage temp. 
room temp
solubility 
H2O: soluble10mg/mL (clear solution)
form 
powder
pka
8.20±0.42(Predicted)
color 
white to beige
Water Solubility 
H2O: 10mg/mL (clear solution)
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0446
Product name
A-419259 trihydrochloride
Purity
≥98% (HPLC)
Packaging
5mg
Price
$213
Updated
2025/07/31
Sigma-Aldrich
Product number
SML0446
Product name
A-419259 trihydrochloride
Purity
≥98% (HPLC)
Packaging
25mg
Price
$894
Updated
2025/07/31
Cayman Chemical
Product number
25605
Product name
A-419259
Purity
≥98%
Packaging
1mg
Price
$81
Updated
2024/03/01
Cayman Chemical
Product number
25605
Product name
A-419259
Purity
≥98%
Packaging
500μg
Price
$35
Updated
2021/12/16
Cayman Chemical
Product number
25605
Product name
A-419259
Purity
≥98%
Packaging
5mg
Price
$199
Updated
2024/03/01
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A 419259 trihydrochloride Chemical Properties,Usage,Production

Description

A-419259 is an inhibitor of Src family kinases, including Src, LCK, Lyn, and Hck (IC50s = 9, <3, <3, and 11.26 nM, respectively)., It is selective for these kinases over c-Abl (IC50 = 3,000 nM) and PKC (IC50 = >33 μM). A-419259 inhibits growth of Philadelphia chromosome-positive (Ph+) K-562 and Meg-01 myeloid leukemia cells (IC50s = 0.1-0.3 and 0.1 μM, respectively), but not Ph- TF-1 and HEL cells. It induces apoptosis in K-562 cells in a concentration-dependent manner. A-419259 (300 nM) inhibits differentiation of murine embryonic stem cells while maintaining pluripotency. It reduces the total number of acute myeloid leukemia (AML) cells, as well as AML stem cells, in the bone marrow and spleen in mouse patient-derived xenograft (PDX) models of AML when administered at a dose of 30 mg/kg twice daily.

Uses

A 419259 Trihydrochloride is the hydrochloride form of A 419259 which is a Src kinase inhibitor and can be used in treatment of chronic myelogenous leukemia, lymphangioleiomyomatosis and tuberous sclerosis.

References

[1] MATTHEW B WILSON. Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr–Abl signal transduction and oncogenesis[J]. Oncogene, 2002, 21 53: 8075-8088. DOI: 10.1038/sj.onc.1206008
[2] T PENE-DUMITRESCU. An inhibitor-resistant mutant of Hck protects CML cells against the antiproliferative and apoptotic effects of the broad-spectrum Src family kinase inhibitor A-419259[J]. Oncogene, 2008, 27 56: 7055-7069. DOI: 10.1038/onc.2008.330
[3] MALCOLM A MEYN. SRC family kinase activity is required for murine embryonic stem cell growth and differentiation.[J]. Molecular Pharmacology, 2005, 68 5: 1320-1330. DOI: 10.1124/mol.104.010231
[4] YORIKO SAITO. A Pyrrolo-Pyrimidine Derivative Targets Human Primary AML Stem Cells in Vivo[J]. Science Translational Medicine, 2013, 5 181. DOI: 10.1126/scitranslmed.3004387

A 419259 trihydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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A 419259 trihydrochloride Suppliers

China 33 United States 9 Global 42
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364042-47-7, A 419259 trihydrochlorideRelated Search:


  • 7-((1r,4r)-4-(4-methylpiperazin-1-yl)cyclohexyl)-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
  • A 419259 trihydrochloride
  • A 419259
  • A419259
  • A-419259
  • RK 20449
  • RK20449
  • RK-20449
  • 7-[Trans-4-(4-methyl-1-piperazinyl)cyclohexyl]-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine trihydrochloride
  • 7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]-5-(4-phenoxyphenyl)-
  • A-419259 HCl
  • 364042-47-7