A 419259 trihydrochloride CAS: 1435934-25-0
MF: C29H34N6O•3HCl
MW: 592.01

A 419259 trihydrochloride (CAS 1435934-25-0)

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Nomi alternativi: A 419259 trihydrochloride is also known as RK-20449.
Applicazione: A 419259 trihydrochloride is an apoptosis inducing agent that inhibits kinases of the Src family, including Src, LCK, Lyn, and Hck.
Numero CAS: 1435934-25-0
Purezza: ≥98%
Peso molecolare: 592.01
Formula molecolare: C29H34N6O•3HCl
Solo per uso in Ricerca. Non previsto per Uso Diagnostico o Terapeutico.
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A 419259 trihydrochloride is an apoptosis inducing agent that inhibits Src family kinases (SFK). The kinases inhibited by A 419259 trihydrochloride include Src, LCK, Lyn, and Hck. A 419259 trihydrochloride is seledcetive for Src family kinases over c-Abl and PKC, with an IC50 of 3,000 nM and > 33 µM, respectively. A 419259 trihydrochloride can induce concentration-dependent apoptosis in K-562 cells. In the bone marrow and spleen of mice xenograft models, A 419259 trihydrochloride was observed to reduce the total number of acute myeloid leukemia cells.


Referenze

1. Wilson et al (2002) Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr-Abl signal transduction and oncogenesis. Oncogene 21 8075.
2. Zhang et al (2004) Src family kinases mediate epidermal growth factor receptor ligand cleavage, proliferation, and invasion of head and neck cancer cells. Cancer Res. 64 6166.
3. Pene-Dumitrescu et al (2008) 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. Oncogene 27 7055.

Aspetto :
Powder or crystalline
Stato fisico :
Solid
Solubilità :
Soluble in DMSO (59.2 mg/ml).
CONSERVAZIONE :
Store at 4° C
IC50 :
Src family kinases (SFK): IC50 = 0.1-0.3 µM
Solo per uso in Ricerca. Non previsto per Uso Diagnostico o Terapeutico.
SMILES :
CN1CCN(CC1)[[email protected]]2CC[[email protected]@H](CC2)n3c4ncnc(c4c(c3)c5ccc(cc5)Oc6ccccc6)N.Cl.Cl.Cl

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A 419259 trihydrochloride (CAS 1435934-25-0)  Citazioni prodotti

Vedi quanti altri hanno usato A 419259 trihydrochloride (CAS 1435934-25-0). Clicca sulla voce per laccesso a PubMed .

Ciatazioni 1 a6 di 6 totali

PMID: # 34675201  Vinel, C.|Rosser, G.|Guglielmi, L.|Constantinou, M.|Pomella, N.|Zhang, X.|Boot, JR.|Jones, TA.|Millner, TO.|Dumas, AA.|Rakyan, V.|Rees, J.|Thompson, JL.|Vuononvirta, J.|Nadkarni, S.|El Assan, T.|Aley, N.|Lin, YY.|Liu, P.|Nelander, S.|Sheer, D.|Merry, CLR.|Marelli-Berg, F.|Brandner, S.|Marino, S.| et al. 2021. Nat Commun. 12: 6130.

PMID: # 31326613  Wilkinson, AC.|Ryan, DJ.|Kucinski, I.|Wang, W.|Yang, J.|Nestorowa, S.|Diamanti, E.|Tsang, JC.|Wang, J.|Campos, LS.|Yang, F.|Fu, B.|Wilson, N.|Liu, P.|Gottgens, B.| et al. 2019. Exp. Hematol.

PMID: # 29019987  Yang, J.|Ryan, DJ.|Wang, W.|Tsang, JC.|Lan, G.|Masaki, H.|Gao, X.|Antunes, L.|Yu, Y.|Zhu, Z.|Wang, J.|Kolodziejczyk, AA.|Campos, LS.|Wang, C.|Yang, F.|Zhong, Z.|Fu, B.|Eckersley-Maslin, MA.|Woods, M.|Tanaka, Y.|Chen, X.|Wilkinson, AC.|Bussell, J.|White, J.|Ramirez-Solis, R.|Reik, W.|Göttgens, B.|Teichmann, SA.|Tam, PPL.|Nakauchi, H.|Zou, X.|Lu, L.|Liu, P.| et al. 2017. Nature. 550: 393-397.

PMID: # 23895624  Zhang, X. et al. 2014. ACS Chem. Biol. 9: 139-46.

PMID: # 25305536  Zhang, X. et al. 2014. Stem cell research. 13: 379-89.

PMID: # 32567735  EMBO J. e103790.

Ciatazioni 1 a6 di 6 totali
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