MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 206185 | Name: Cenisertib

Description:

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

Cenisertib, also known as AS-703569 or R763; is an orally bioavailable, synthetic, small-molecule multi-Aurora kinase inhibitor with potential antineoplastic activity. Cenisertib selectively binds to and inhibits multiple Aurora kinases (AKs), which may result in the inhibition of cell division and proliferation, and the induction of apoptosis in tumor cells that overexpress AKs. Overexpressed in certain tumor cell types, AKs, a family of serine-threonine kinases, are important regulators of cell division and proliferation that are involved in controlling chromatid segregation.

Chemical Structure

Cenisertib
Cenisertib
CAS#871357-89-0

Theoretical Analysis

MedKoo Cat#: 206185

Name: Cenisertib

CAS#: 871357-89-0

Chemical Formula: C24H30FN7O

Exact Mass: 451.2496

Molecular Weight: 451.54

Elemental Analysis: C, 63.84; H, 6.70; F, 4.21; N, 21.71; O, 3.54

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
Bulk Inquiry
Related CAS #
No Data
Synonym
R763; R 763; R-763; AS703569; AS-703569; AS 703569; MSC1992371A; Cenisertib.
IUPAC/Chemical Name
(1S,2S,3R,4R)-3-((5-fluoro-2-((3-methyl-4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)bicyclo[2.2.1]hept-5-ene-2-carboxamide
InChi Key
KSOVGRCOLZZTPF-QMKUDKLTSA-N
InChi Code
InChI=1S/C24H30FN7O/c1-14-11-17(5-6-19(14)32-9-7-31(2)8-10-32)28-24-27-13-18(25)23(30-24)29-21-16-4-3-15(12-16)20(21)22(26)33/h3-6,11,13,15-16,20-21H,7-10,12H2,1-2H3,(H2,26,33)(H2,27,28,29,30)/t15-,16+,20+,21-/m1/s1
SMILES Code
O=C([C@H]1[C@](C2)([H])C=C[C@]2([H])[C@H]1NC3=NC(NC4=CC=C(N5CCN(C)CC5)C(C)=C4)=NC=C3F)N
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, not in water
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
More Info
        

Preparing Stock Solutions

The following data is based on the product molecular weight 451.54 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
1: Illert AL, Seitz AK, Rummelt C, Kreutmair S, Engh RA, Goodstal S, Peschel C, Duyster J, von Bubnoff N. Inhibition of Aurora kinase B is important for biologic activity of the dual inhibitors of BCR-ABL and Aurora kinases R763/AS703569 and PHA-739358 in BCR-ABL transformed cells. PLoS One. 2014 Nov 26;9(11):e112318. doi: 10.1371/journal.pone.0112318. eCollection 2014. PubMed PMID: 25426931; PubMed Central PMCID: PMC4245092. 2: Mita M, Gordon M, Rejeb N, Gianella-Borradori A, Jego V, Mita A, Sarantopoulos J, Sankhala K, Mendelson D. A phase l study of three different dosing schedules of the oral aurora kinase inhibitor MSC1992371A in patients with solid tumors. Target Oncol. 2014 Sep;9(3):215-24. doi: 10.1007/s11523-013-0288-3. Epub 2013 Jul 6. PubMed PMID: 23832397. 3: Graux C, Sonet A, Maertens J, Duyster J, Greiner J, Chalandon Y, Martinelli G, Hess D, Heim D, Giles FJ, Kelly KR, Gianella-Borradori A, Longerey B, Asatiani E, Rejeb N, Ottmann OG. A phase I dose-escalation study of MSC1992371A, an oral inhibitor of aurora and other kinases, in advanced hematologic malignancies. Leuk Res. 2013 Sep;37(9):1100-6. doi: 10.1016/j.leukres.2013.04.025. Epub 2013 Jun 5. PubMed PMID: 23746966. 4: Raymond E, Alexandre J, Faivre S, Goldwasser F, Besse-Hammer T, Gianella-Borradori A, Jego V, Trandafir L, Rejeb N, Awada A. A phase I schedule dependency study of the aurora kinase inhibitor MSC1992371A in combination with gemcitabine in patients with solid tumors. Invest New Drugs. 2014 Feb;32(1):94-103. doi: 10.1007/s10637-013-9950-y. Epub 2013 Mar 29. PubMed PMID: 23539344. 5: Romanelli A, Clark A, Assayag F, Chateau-Joubert S, Poupon MF, Servely JL, Fontaine JJ, Liu X, Spooner E, Goodstal S, de Cremoux P, Bièche I, Decaudin D, Marangoni E. Inhibiting aurora kinases reduces tumor growth and suppresses tumor recurrence after chemotherapy in patient-derived triple-negative breast cancer xenografts. Mol Cancer Ther. 2012 Dec;11(12):2693-703. doi: 10.1158/1535-7163.MCT-12-0441-T. Epub 2012 Sep 25. PubMed PMID: 23012245. 6: Curtin ML, Heyman HR, Frey RR, Marcotte PA, Glaser KB, Jankowski JR, Magoc TJ, Albert DH, Olson AM, Reuter DR, Bouska JJ, Montgomery DA, Palma JP, Donawho CK, Stewart KD, Tse C, Michaelides MR. Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4750-5. doi: 10.1016/j.bmcl.2012.05.067. Epub 2012 May 26. PubMed PMID: 22695126. 7: Martinelli G, Iacobucci I, Papayannidis C, Soverini S. New targets for Ph+ leukaemia therapy. Best Pract Res Clin Haematol. 2009 Sep;22(3):445-54. doi: 10.1016/j.beha.2009.08.002. Review. PubMed PMID: 19959093. 8: McLaughlin J, Markovtsov V, Li H, Wong S, Gelman M, Zhu Y, Franci C, Lang D, Pali E, Lasaga J, Low C, Zhao F, Chang B, Gururaja TL, Xu W, Baluom M, Sweeny D, Carroll D, Sran A, Thota S, Parmer M, Romane A, Clemens G, Grossbard E, Qu K, Jenkins Y, Kinoshita T, Taylor V, Holland SJ, Argade A, Singh R, Pine P, Payan DG, Hitoshi Y. Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen. J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113. doi: 10.1007/s00432-009-0641-1. PubMed PMID: 19609559.

View History

Cabozantinib free base

Cabozantinib free base

New Featured