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

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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