A-419259 HCl
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MedKoo CAT#: 555204

CAS#: 364042-47-7 (free base)

Description: A-419259 is a potent inhibitor of Src family kinases. IC50 values for src, lck, blk, csk, fyn and lyn range between 15 and 50 nM.


Chemical Structure

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A-419259 HCl
CAS# 364042-47-7 (free base)

Theoretical Analysis

MedKoo Cat#: 555204
Name: A-419259 HCl
CAS#: 364042-47-7 (free base)
Chemical Formula: C29H37Cl3N6O
Exact Mass:
Molecular Weight: 592.006
Elemental Analysis: C, 58.84; H, 6.30; Cl, 17.96; N, 14.20; O, 2.70

Price and Availability

Size Price Availability Quantity
5.0mg USD 350.0 2 Weeks
25.0mg USD 950.0 2 Weeks
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Related CAS #: 364042-47-7 (free base)    

Synonym: A-419259 trihydrochloride; A419259; A 419259; RK20449; RK-20449; RK 20449

IUPAC/Chemical Name: 7-[Trans-4-(4-methyl-1-piperazinyl)cyclohexyl]-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine trihydrochloride

InChi Key: ALRMEQIQFCUAMR-KOONDFAVSA-N

InChi Code: 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-;;;

SMILES Code: NC1=C2C(N([C@H]3CC[C@H](N4CCN(C)CC4)CC3)C=C2C5=CC=C(OC6=CC=CC=C6)C=C5)=NC=N1.[H]Cl.[H]Cl.[H]Cl

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 592.006 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Zhang X, Simerly C, Hartnett C, Schatten G, Smithgall TE. Src-family tyrosine kinase activities are essential for differentiation of human embryonic stem cells. Stem Cell Res. 2014 Nov;13(3 Pt A):379-89. doi: 10.1016/j.scr.2014.09.007. Epub 2014 Sep 30. PubMed PMID: 25305536; PubMed Central PMCID: PMC4252886.

2: Je DW, O YM, Ji YG, Cho Y, Lee DH. The inhibition of SRC family kinase suppresses pancreatic cancer cell proliferation, migration, and invasion. Pancreas. 2014 Jul;43(5):768-76. doi: 10.1097/MPA.0000000000000103. PubMed PMID: 24763074.

3: Parker LJ, Taruya S, Tsuganezawa K, Ogawa N, Mikuni J, Honda K, Tomabechi Y, Handa N, Shirouzu M, Yokoyama S, Tanaka A. Kinase crystal identification and ATP-competitive inhibitor screening using the fluorescent ligand SKF86002. Acta Crystallogr D Biol Crystallogr. 2014 Feb;70(Pt 2):392-404. doi: 10.1107/S1399004713028654. Epub 2014 Jan 29. PubMed PMID: 24531473.

4: Zhang X, Meyn MA 3rd, Smithgall TE. c-Yes tyrosine kinase is a potent suppressor of ES cell differentiation and antagonizes the actions of its closest phylogenetic relative, c-Src. ACS Chem Biol. 2014 Jan 17;9(1):139-46. doi: 10.1021/cb400249b. Epub 2013 Aug 15. PubMed PMID: 23895624; PubMed Central PMCID: PMC3875617.

5: Dincer S, Cetin KT, Onay-Besikci A, Ölgen S. Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors. J Enzyme Inhib Med Chem. 2013 Oct;28(5):1080-7. doi: 10.3109/14756366.2012.715288. Epub 2012 Sep 7. PubMed PMID: 22957720.

6: Pene-Dumitrescu T, Peterson LF, Donato NJ, Smithgall TE. 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 Nov 27;27(56):7055-69. doi: 10.1038/onc.2008.330. Epub 2008 Sep 15. PubMed PMID: 18794796; PubMed Central PMCID: PMC2738638.

7: Meyn MA 3rd, Schreiner SJ, Dumitrescu TP, Nau GJ, Smithgall TE. SRC family kinase activity is required for murine embryonic stem cell growth and differentiation. Mol Pharmacol. 2005 Nov;68(5):1320-30. Epub 2005 Jun 28. PubMed PMID: 15985613.

8: Zhang Q, Thomas SM, Xi S, Smithgall TE, Siegfried JM, Kamens J, Gooding WE, Grandis JR. SRC family kinases mediate epidermal growth factor receptor ligand cleavage, proliferation, and invasion of head and neck cancer cells. Cancer Res. 2004 Sep 1;64(17):6166-73. PubMed PMID: 15342401.

9: Wilson MB, Schreiner SJ, Choi HJ, Kamens J, Smithgall TE. 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. PubMed PMID: 12444544.