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Cat. No.: HY-120534

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BPR1K653 hydrochloride

Name: BPR1K653 hydrochloride
Brand: MedChemExpress
SKU: HY-120534
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BPR1K653 hydrochloride is a pan-Aurora kinase inhibitor, with an IC₅₀ of 124.0 nM against Aurora-A and an IC₅₀ of 45.0 nM against Aurora-B. BPR1K653 hydrochloride induces endoreduplication, apoptosis and antiproliferative activity in cancer cells. BPR1K653 hydrochloride can be used in research related to colon cancer and multidrug-resistant cancers.

For research use only. We do not sell to patients.

CAS No.: 1192754-07-6
Formula: C₃₀H₃₀Cl₂N₆O₂
Molecular Weight:577.50

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

BPR1K653 hydrochloride Chemical Structure

CAS No.: 1192754-07-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]^[2]

Aurora A

124.0 nM (IC₅₀)

Aurora B

45.0 nM (IC₅₀)

All Aurora Kinase Isoforms :

In Vitro

Anti-cancerCell Cycle RegulationApoptosisOthers

Anti-cancer

BPR1K653 (0-10000 nM; administered 1 h after 24 h pretreatment with Nocodazole (HY-13520)) hydrochloride preferentially inhibits Aurora-B (Thr232) autophosphorylation over Aurora-A (Thr288) autophosphorylation in Nocodazole-arrested human colon cancer HCT116 cells, with IC₅₀ values of 23.7 nM and 73.4 nM, respectively^[1].
BPR1K653 hydrochloride potently inhibits the viability of human colon cancer cell line HCT116 (IC₅₀ = 70 nM), and exhibits low toxicity toward normal human skin fibroblast cell line Detroit 551 (IC₅₀ = 3.1 μM)^[1].
BPR1K653 (10-1000 nM) hydrochloride inhibits aurora kinase activity in HCT116 colon cancer cells, as evidenced by concentration-dependent decreases in the levels of phosphorylated Aurora-A, Aurora-B, Aurora-C and phosphorylated histone H3^[2].
BPR1K653 (third-generation culture cycle) hydrochloride potently inhibits the proliferation of various human cancer cell lines, regardless of tissue origin, p53 status, or the expression levels of MDR1 and MRP1 efflux pumps, with an IC₅₀ value range of 4 nM to 135 nM^[2].

Anti-cancer

Cell Cycle Regulation

BPR1K653 (10-20 h after thymidine release) hydrochloride significantly reduces the mitotic index of synchronized HeLa human cervical cancer cells^[1].
BPR1K653 hydrochloride is a potent and selective pan-aurora kinase inhibitor, with an IC₅₀ value of 124 nM against Aurora-A and 45 nM against Aurora-B, and exhibits extremely low activity against a panel of non-aurora kinases^[2].
BPR1K653 (48 h) hydrochloride induces endoreplication and polyploidy in KB, MDR1-positive KB-VIN10 and HONE-1 human cancer cells in a concentration-dependent manner^[2].
BPR1K653 (48 h) hydrochloride downregulates the expressions of phosphorylated histone H3 and cyclin B1 in a concentration-dependent manner in KB, MDR1-positive KB-VIN10 and HONE-1 human cancer cells^[2].

Anti-cancer

Apoptosis

BPR1K653 (48 h for Annexin-V, 60 h for caspase-3/-7 imaging, 72 h for TUNEL and PARP cleavage) hydrochloride induces apoptosis in human KB, MDR1-positive KB-VIN10, and HONE-1 cancer cells, which is confirmed by Annexin-V staining, caspase activation, DNA fragmentation, and PARP cleavage^[2].

Others

BPR1K653 hydrochloride is a pan-Aurora kinase inhibitor, with stronger inhibitory activity against purified Aurora-B kinase (IC₅₀ = 45.0 nM) than against purified Aurora-A kinase (IC₅₀ = 124.0 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

HCT116 human colon carcinoma cells
Concentration:

10-1000 nM
Incubation Time:

1 h (after 24 h Nocodazole pretreatment)
Result:

Inhibited autophosphorylation of Aurora-A (Thr288) with an IC₅₀ of 73.4 nM.
Showed stronger inhibition of Aurora-B (Thr232) autophosphorylation with an IC₅₀ of 23.7 nM.
Resulted in a cellular Aurora-A/B IC₅₀ ratio of 3.1/1.

In Vivo

Anti-cancerApoptosisCell Cycle Regulation

Anti-cancer

Apoptosis

Cell Cycle Regulation

BPR1K653 (15 mg/kg; i.p.; 5 days/week; 2 consecutive weeks) inhibits KB cervical cancer xenograft growth by ~73%, reduces Aurora kinase activity, and induces tumor cell apoptosis in nude mice^[2].

Anti-cancer

BPR1K653 (15 mg/kg; i.p.; 5 days/week; 3 consecutive weeks) hydrochloride inhibits MDR1-positive KB-VIN10 cervical cancer xenograft growth by ~50% in nude mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Nude mice (male, 5-6 weeks old)^[2]
Dosage:

15 mg/kg
Administration:

i.p.; 5 days/week; 2 consecutive weeks
Result:

Reduced the percentage of phosphor-Histone H3 positive tumor cells to 10% from controls.
Reduced tumor volume by ~73% compared to controls on day 30.
Induced 55% apoptotic cells in tumor tissue at 12 days post-treatment compared to controls.
Caused body weight loss of less than 10% relative to controls.

Animal Model:

Nude mice (male, 5-6 weeks old)^[2]
Dosage:

15 mg/kg
Administration:

i.p.; 5 days/week; 3 consecutive weeks
Result:

Reduced tumor volume by ~50% compared to controls on day 42.
Caused body weight loss of less than 10% relative to controls.

Related Protocols :

Chemical Information

CAS No. 1192754-07-6
Molecular Weight 577.50
Formula C₃₀H₃₀Cl₂N₆O₂
SMILES

O=C(NC1=CC=C(C=C1)CCNC2=C3C(OC(C4=CC=CC=C4)=C3Cl)=NC=N2)NC5=CC=CC=C5CN(C)C.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Ke YY, et al. Design and synthesis of BPR1K653 derivatives targeting the back pocket of Aurora kinases for selective isoform inhibition. European journal of medicinal chemistry. 2018 May 10;151:533-545.

[2]. Cheung CH, et al. BPR1K653, a novel Aurora kinase inhibitor, exhibits potent anti-proliferative activity in MDR1 (P-gp170)-mediated multidrug-resistant cancer cells. PloS one. 2011;6(8):e23485.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
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- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
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BPR1K653 hydrochloride

All Aurora Kinase Isoforms

Biological Activity

Description

IC50 & Target

In Vitro

In Vivo

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs