TozasertibA potent and selective pan-ARK inhibitor

Tozasertib (CAS 639089-54-6)

Tozasertib | CAS 639089-54-6 is rated 5.0 out of 5 by 1.
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Synonym: MK0457; VX 680; MK 0457
Application: A potent and selective pan-ARK inhibitor
CAS Number: 639089-54-6
Purity: ≥98%
Molecular Weight: 464.59
Molecular Formula: C23H28N8OS
* Refer to Certificate of Analysis for lot specific data (including water content).
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Tozasertib is a potent pan-ARK inhibitor but favors ARK-1 (Ki = 0.6 nM) over ARK-2 (Ki = 18 nM) or ARK-3 (Ki = 4.6 nM). It shows selectivity against a panel of more than 190 different protein kinases. Tozasertib effectively inhibits proliferation of several different cell lines of clear cell renal carcinoma (IC50 < 10μM), inhibiting H3 histone phosphorylation and increasing apoptosis. By depleting ARK activity, tozasertib disrupts bipolar spindle formation during mitosis, arresting cell cycle progression at the G2/M phase.


References

1. Pollard, J.R., et al. 2009. J. Med. Chem. 52: 2629-2651. PMID: 19320489
2. Li, Y., et al. 2010. Am J Transl Res. 2: 296-308. PMID: 20589168

Physical State :
Solid
Solubility :
Soluble in plain water (10-30 µM), DMSO (100 mg/ml), ethanol (<1 mg/ml) at 25 °C, and methanol.
Storage :
Store at -20° C
Melting Point :
168-174° C
Density :
~1.41 g/cm3 (Predicted)
Refractive Index :
n20D 1.71 (Predicted)
IC50 :
Aurora A : IC50 = 0.6 nM; Aurora B: IC50 = 18 nM; Aurora C : IC50 = 4.6 nM; different ATC cells: IC50 = 25- 150 nM; inhibits the growth of cells expressing wild type and mutated BCR-ABL, including T315I: IC50 = 200 nM
Ki Data :
ABL kinase: Ki= 30 nM; imatinib-resistant ABL mutant (T315I) kinase: Ki= 42 nM; Flt-3: Ki= 30 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
5494449
MDL Number :
MFCD13185152
SMILES :
CC1=CC(=NN1)NC2=NC(=NC(=C2)N3CCN(CC3)C)SC4=CC=C(C=C4)NC(=O)C5CC5

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Certificate of Analysis

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Tozasertib  Product Citations

See how others have used Tozasertib. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 23824559  Kim, KC. et al. 2013. Neurochemical research. 38: 1960-72.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Yin Yin, Y. et al. (PubMed 25543471) investigated the effect of VX 680 (Tozasertib; MK0457; MK 0457), an aurora inhibitor, on proliferation and apoptosis of K562, KCL22 cell lines and CD34+ cells from chronic myeloid leukemia (CML) patients in vitro. VX-680 treatment significantly induced apoptosis of K562 and KCL22 cells and inhibited the cell proliferation of all three cell lines in a concentration-dependent manner. -SCBT Publication Review
Date published: 2015-05-28
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