A 419259 trihydrochloride


Catalog No. size PriceQuantity
M6696-2 2mg solid $242
M6696-10 10mg solid $956

Description

A 419259 trihydrochloride is a second-generation pyrrolo-pyrimidine designed to enhance selectivity towards the Src family relative to other cytoplasmic tyrosine kinases.

Product information

CAS Number: 1435934-25-0

Molecular Weight: 592.00

Formula: C29H37Cl3N6O

Chemical Name: 7-((1r,4r)-4-(4-methylpiperazin-1-yl)cyclohexyl)-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine trihydrochloride

Smiles: Cl.Cl.Cl.CN1CCN(CC1)[C@@H]1CC[C@H](CC1)N1C=C(C2=C(N)N=CN=C12)C1C=CC(=CC=1)OC1C=CC=CC=1

InChiKey: ALRMEQIQFCUAMR-KOONDFAVSA-N

InChi: InChI=1S/C29H34N6O.3ClH/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);3*1H/t22-,23-;;;

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

A 419259 Trihydrochloride is a second-generation pyrrolo-pyrimidine designed to enhance selectivity towards the Src family relative to other cytoplasmic tyrosine kinases. A 419259 inhibits K-562 cells with an IC50 between 0.1 and 0.3 μM, and Meg-01 proliferation with an IC50 of approximately 0.1 μM. A 419259 also potently induces apoptosis in K-562 cells beginning at 0.1 μM and increasing in a dose-dependent manner. PP2 inhibits Src kinase autophosphorylation in both Ph+ cell lines (K-562 and Meg-01) with an IC50 between 3 and 10 μM, while A 419259 blocks kinase activation between 0.1 and 0.3 μM. A 419259 strongly inhibits DAGM/Bcr-Abl cell proliferation in the absence of IL-3 with an IC50 between 0.1 and 0.3 μM. A 419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, and blocks proliferation and induces apoptosis in CML cell lines. A 419259 inhibits overall SFK activity in K562 and other CML cell lines with an IC50 value of 0.1-0.3 μM.

References:

  1. A J Vázquez, B I Diamond, H C Sabelli. Differential effects of phenobarbital and pentobarbital on isolated nervous tissue. Epilepsia.1975 Nov;16(4):601-8.
  2. Wilson MB, et al. Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr-Abl signal transduction and oncogenesis. Oncogene. 2002 Nov 21;21(53):8075-88.
  3. Pene-Dumitrescu T, et al. 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 (2008) 27, 7055-7069

Products are for research use only. Not for human use.

Payment & Security

American Express Diners Club Discover JCB Mastercard PayPal Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed