Aurora A Inhibitor I
- Product Name
- Aurora A Inhibitor I
- CAS No.
- 1158838-45-9
- Chemical Name
- Aurora A Inhibitor I
- Synonyms
- Aurora A-IN-10;Aurora A Inhibitor I;TC-S 7010 Aurora A Inhibitor;Aurora A Inhibitor I USP/EP/BP;TC-S 7010 (Aurora A Inhibitor I);Aurora A Inhibitor I (TC-S 7010);Aurora-A Inhibitor I >=98% (HPLC);N-(2-Chlorophenyl)-4-((2-((4-(2-(4-ethylpiperazin-1-yl)-2-oxoethyl)-phenyl)amino)-5-fluoropyri;N-(2-Chlorophenyl)-4-((2-((4-(2-(4-ethylpiperazin-1-yl)-2-oxoethyl)-phenyl)amino)-5-fluoropyrimid;N-(2-Chlorophenyl)-4-(2-(4-(2-(4-ethylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)benzamide
- CBNumber
- CB62506281
- Molecular Formula
- C31H31ClFN7O2
- Formula Weight
- 588.07
- MOL File
- 1158838-45-9.mol
Aurora A Inhibitor I Property
- Density
- 1.362
- storage temp.
- 2-8°C
- solubility
- DMSO: soluble10mg/mL, clear
- form
- powder
- color
- white to beige
- InChIKey
- AKSIZPIFQAYJGF-UHFFFAOYSA-N
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML0882
- Product name
- Aurora-A Inhibitor I
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $165
- Updated
- 2024/03/01
- Product number
- SML0882
- Product name
- Aurora-A Inhibitor I
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $657
- Updated
- 2024/03/01
- Product number
- 21600
- Product name
- Aurora A Inhibitor I
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 21600
- Product name
- Aurora A Inhibitor I
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $139
- Updated
- 2024/03/01
- Product number
- 21600
- Product name
- Aurora A Inhibitor I
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $243
- Updated
- 2024/03/01
Aurora A Inhibitor I Chemical Properties,Usage,Production
Uses
TC-S 7010 is a selective Aurora A inhibitor.
Definition
ChEBI: N-(2-chlorophenyl)-4-[[2-[4-[2-(4-ethyl-1-piperazinyl)-2-oxoethyl]anilino]-5-fluoro-4-pyrimidinyl]amino]benzamide is a member of benzamides.
Biological Activity
aurora a inhibitor i is a novel, potent, and selective inhibitor of aurora a .aurora kinases are reported to be required for mitosis and to complete cell division. because of this, aurora kinase inhibitors have been investigated extensively as potential anticancer therapeutic agents. the two major aurora kinases (aurora a and aurora b) are closely related in kinase domain sequence (71% identical).
in vitro
aurora a inhibitor i was tested against wild-type kinase and two mutants (aurora a (t217e) and aurora b (e161t)). the inhibitory potencies of aurora a inhibitor i was strongly affected by the single amino acid substitutions. for either aurora kinase, the presence of threonine allowed potent inhibition, while for glutamic acid variants, there was a approximately 100-fold shift in ic50, which supported the “gating” role for this residue. the aurora b binding pocket was enlarged by the e161t mutation, while the pocket in aurora a was closed by the t217e mutation. aurora a inhibitor i was exceptionally selective aurora a inhibitors, as shown by no inhibition on aurora b or cdks was observed in cellular assays [1].
IC 50
3.4 nm.
storage
Store at +4°C
References
[1] aliagas-martin i,burdick d,corson l,dotson j,drummond j,fields c,huang ow,hunsaker t,kleinheinz t,krueger e,liang j,moffat j,phillips g,pulk r,rawson te,ultsch m,walker l,wiesmann c,zhang b,zhu by,cochran ag. a class of 2,4-bisanilinopyrimidine aurora a inhibitors with unusually high selectivity against aurora b. j med chem.2009 may 28;52(10):3300-7.