SAR-020106

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406347

CAS#: 1184843-57-9

Description: SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion. Biomarker studies have shown that SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion both in vitro and in vivo. SAR-020106 represents a novel class of CHK1 inhibitors that can enhance antitumor activity with selected anticancer drugs in vivo and may therefore have clinical utility.


Price and Availability

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SAR-020106 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406347
Name: SAR-020106
CAS#: 1184843-57-9
Chemical Formula: C19H19ClN6O
Exact Mass: 382.13089
Molecular Weight: 382.85
Elemental Analysis: C, 59.61; H, 5.00; Cl, 9.26; N, 21.95; O, 4.18


Synonym: SAR020106; SAR020106; SAR 020106; SAR20106; SAR20106; SAR 20106.

IUPAC/Chemical Name: (R)-5-((8-chloroisoquinolin-3-yl)amino)-3-((1-(dimethylamino)propan-2-yl)oxy)pyrazine-2-carbonitrile

SMILES Code: N#CC1=NC=C(NC2=CC3=C(C=N2)C(Cl)=CC=C3)N=C1O[C@H](C)CN(C)C


Technical Data

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:
0 – 4 C for short term (weeks to 1 month) or -20 C for long terms (months to years).

Solubility:
soluble in DMSO, not soluble in water.

Shelf Life:
>2 years if stored properly.

Drug Formulation:
Stock solution storage:

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

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

1: Touchefeu Y, Khan AA, Borst G, Zaidi SH, McLaughlin M, Roulstone V, Mansfield D, Kyula J, Pencavel T, Karapanagiotou EM, Clayton J, Federspiel MJ, Russell SJ, Garrett M, Collins I, Harrington KJ. Optimising measles virus-guided radiovirotherapy with external beam radiotherapy and specific checkpoint kinase 1 inhibition. Radiother Oncol. 2013 Jul;108(1):24-31. doi: 10.1016/j.radonc.2013.05.036. Epub 2013 Jul 9. PubMed PMID: 23849174.

2: Borst GR, McLaughlin M, Kyula JN, Neijenhuis S, Khan A, Good J, Zaidi S, Powell NG, Meier P, Collins I, Garrett MD, Verheij M, Harrington KJ. Targeted radiosensitization by the Chk1 inhibitor SAR-020106. Int J Radiat Oncol Biol Phys. 2013 Mar 15;85(4):1110-8. doi: 10.1016/j.ijrobp.2012.08.006. Epub 2012 Sep 14. PubMed PMID: 22981708.

3: Reader JC, Matthews TP, Klair S, Cheung KM, Scanlon J, Proisy N, Addison G, Ellard J, Piton N, Taylor S, Cherry M, Fisher M, Boxall K, Burns S, Walton MI, Westwood IM, Hayes A, Eve P, Valenti M, de Haven Brandon A, Box G, van Montfort RL, Williams DH, Aherne GW, Raynaud FI, Eccles SA, Garrett MD, Collins I. Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. J Med Chem. 2011 Dec 22;54(24):8328-42. doi: 10.1021/jm2007326. Epub 2011 Nov 23. PubMed PMID: 22111927; PubMed Central PMCID: PMC3241339.

4: Walton MI, Eve PD, Hayes A, Valenti M, De Haven Brandon A, Box G, Boxall KJ, Aherne GW, Eccles SA, Raynaud FI, Williams DH, Reader JC, Collins I, Garrett MD. The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106. Mol Cancer Ther. 2010 Jan;9(1):89-100. doi: 10.1158/1535-7163.MCT-09-0938. Epub 2010 Jan 6. PubMed PMID: 20053762.