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Safety Information

SML2568

Sigma-Aldrich

XMD8-87

≥98% (HPLC)

Synonym(s):

5,11-Dihydro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-11-methyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one, ACK1-B19

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About This Item

Empirical Formula (Hill Notation):
C24H27N7O2
CAS Number:
1234480-46-6
Molecular Weight:
445.52
MDL number:
MFCD30742941
UNSPSC Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Biochem/physiol Actions

XMD8-87 is a potent and selective inhibitor of Ack1 (Activated CDC42 kinase 1, TNK2), a kinase that regulates cellular attachment and migration and whose over-expression correlates with a more invasive phenotype of cancer cells and predisposition of primary tumor cells to metastasis. XMD8-87 had a Kd of 15 nM against ACK1 and was also found to inhibit murine Ba/F3 tumor cells having leukemia-associated TNK2 mutations. It inhibited TNK2 D163E cells with an IC50 value of 38 nM and TNK2 R806Q cells with an IC50 value of 113 nM.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

JAN Code

SML2568-5MG:
SML2568-25MG:
SML2568-VAR:
SML2568-BULK:

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Development and Repurposing of Small-Molecule Kinase Inhibitors to Target Novel Leukemogenic TNK2 Mutations
Julia EM, Abel LM, Jinhua W, et al.
Blood, 124 (21), 435-435 (2014)
Chandrasekhar V Miduturu et al.
Chemistry & biology, 18(7), 868-879 (2011-08-02)
Selective protein kinase inhibitors have only been developed against a small number of kinase targets. Here we demonstrate that "high-throughput kinase profiling" is an efficient method for the discovery of lead compounds for established as well as unexplored kinase targets.
Julia E Maxson et al.
Cancer research, 76(1), 127-138 (2015-12-19)
The amount of genomic information about leukemia cells currently far exceeds our overall understanding of the precise genetic events that ultimately drive disease development and progression. Effective implementation of personalized medicine will require tools to distinguish actionable genetic alterations within

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