IBPR002
IBPR002 is an inhibitor of Aurora kinase A and Aurora kinase B, with IC50 values of 41 nM and 17 nM, respectively. IBPR002 disrupts the nucleation and bundling of kinetochore microtubules, impairs the bipolarity of mitotic spindles, and promotes the binding of non-phosphorylated hepatoma up-regulated protein (HURP) to microtubules derived from the mother centrosome. IBPR002 reduces tumorigenesis levels in a colorectal cancer xenograft model using athymic nude mice. IBPR002 is applicable for research related to colorectal cancer.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 1192754-38-3
- 화학식: C34H36N6O4
- 분자량:592.70
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocol
- 순도&문서
- References
-
Help & FAQs
All Aurora Kinase Isoforms
More
Biological Activity
제품 설명
IC50 & Target
[1]|
Aurora A 41 nM (IC50) |
Aurora B 17 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | EC50 |
195 nM
Compound: 35, IBPR002
|
Antiproliferative activity against human HCT116 cells
Antiproliferative activity against human HCT116 cells
|
[PMID: 23808327] |
In Vitro
IBPR002 (1.0 μM; 13 h) disrupts bipolar spindle formation and restricts unphosphorylated HURP to the minus ends of centrosomal microtubules, inducing three distinct mitotic phenotypes in HeLa cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HeLa cells
-
Concentration:1.0 μM
-
Incubation Time:13 h (after thymidine release)
-
Result:Induced three distinct HURP localization phenotypes: ~20% of cells showed a monoastral spindle with HURP surrounding unseparated centrosomes (Phenotype-1), the majority showed HURP associated with centrosomal microtubules projecting toward chromosomes from one separated centrosome (Phenotype-2) or both separated centrosomes (Phenotype-3).
Disrupted bipolar spindle formation.
Restricted HURP to the minus ends of centrosomal microtubules, unlike control cells where HURP localizes to both ends of microtubules.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:athymic nude (male)[1]
-
Dosage:50 mg/kg
-
Administration:i.v.; five daily doses per week; two consecutive weeks
-
Result:Significantly inhibited growth of xenograft colorectal cancer cells, with mean tumor volume at study end being substantially lower than vehicle control levels.
Chemical Information
-
CAS No. 1192754-38-3
-
분자량 592.70
-
화학식 C34H36N6O4
-
SMILES
O=C(NC=1C=CC=CC1)NC2=CC=C(C=C2)CCNC=3N=CN=C4OC(=CC43)C=5C=CC(OCCN6CCC(O)CC6)=CC5
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IBPR002 Related Classifications
HY-165369 Related Classifications
Powered by Bioz