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Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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SKU | Size | Availability | Price | Qty |
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B414286-5mg | 5mg | In stock | $157.90 | |
B414286-10mg | 10mg | In stock | $256.90 | |
B414286-25mg | 25mg | In stock | $513.90 | |
B414286-50mg | 50mg | In stock | $781.90 | |
B414286-100mg | 100mg | In stock | $1,286.90 |
Serine/threonin kinase Inhibitors
Specifications & Purity | ≥98% |
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Biochemical and Physiological Mechanisms | BAY-1816032 is a potent and oral available inhibitor of budding uninhibited by benzimidazoles 1 (BUB1) kinase with IC50 of 6.1 nM for recombinant catalytic domain of human BUB1. BAY-1816032 has antitumor activity. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | Information BAY-1816032 BAY-1816032 is a potent and oral available inhibitor of budding uninhibited by benzimidazoles 1 (BUB1) kinase with IC50 of 6.1 nM for recombinant catalytic domain of human BUB1. BAY-1816032 has antitumor activity. Targets BUB1 (Cell-free assay) 6.1 nM In vitro BAY 1816032 is a novel, bioavailable inhibitor of the catalytical activity of the mitotic checkpoint protein BUB1, which is involved in centromere cohesion and attachment error correction. Inhibition of BUB1 sensitizes tumor cells towards paclitaxel and docetaxel, and towards ATR inhibitors and PARP inhibitiors. In vivo In xenograft models of triple-negative breast cancer BAY 1816032 in combination with paclitaxel or olaparib strongly delays outgrowth of tumors under treatment as compared to paclitaxel or olaparib single agents. Cell Research(from reference) Cell lines:HeLa, SUM-149, MDA-MB-436, NCI-H1299, 22RV1, H4 cells. Concentrations:0.1 μM to 10 μM Incubation Time:4 h, 24 h, 48 h, 72 h, 96 h |
ALogP | 4.294 |
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HBD Count | 2 |
Rotatable Bond | 10 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 2-[3,5-difluoro-4-[[3-[5-methoxy-4-[(3-methoxypyridin-4-yl)amino]pyrimidin-2-yl]indazol-1-yl]methyl]phenoxy]ethanol |
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INCHI | InChI=1S/C27H24F2N6O4/c1-37-23-13-30-8-7-21(23)32-26-24(38-2)14-31-27(33-26)25-17-5-3-4-6-22(17)35(34-25)15-18-19(28)11-16(12-20(18)29)39-10-9-36/h3-8,11-14,36H,9-10,15H2,1-2H3,(H,30,31,32,33) |
InChi Key | QVOGVAVHOLLLAZ-UHFFFAOYSA-N |
Canonical SMILES | COC1=CN=C(N=C1NC2=C(C=NC=C2)OC)C3=NN(C4=CC=CC=C43)CC5=C(C=C(C=C5F)OCCO)F |
Isomeric SMILES | COC1=CN=C(N=C1NC2=C(C=NC=C2)OC)C3=NN(C4=CC=CC=C43)CC5=C(C=C(C=C5F)OCCO)F |
PubChem CID | 118958833 |
Molecular Weight | 534.51 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
H2329056 | Certificate of Analysis | Aug 10, 2023 | B414286 |
H2329057 | Certificate of Analysis | Aug 10, 2023 | B414286 |
H2329058 | Certificate of Analysis | Aug 10, 2023 | B414286 |
H2329059 | Certificate of Analysis | Aug 10, 2023 | B414286 |
H2329149 | Certificate of Analysis | Aug 10, 2023 | B414286 |
H2329589 | Certificate of Analysis | Aug 10, 2023 | B414286 |
H2329597 | Certificate of Analysis | Aug 10, 2023 | B414286 |
H2329602 | Certificate of Analysis | Aug 10, 2023 | B414286 |
H2329621 | Certificate of Analysis | Aug 10, 2023 | B414286 |
H2329701 | Certificate of Analysis | Aug 10, 2023 | B414286 |
Solubility | Solubility (25°C) In vitro DMSO: 50 mg/mL (93.54 mM); Water: Insoluble; Ethanol: Insoluble; |
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DMSO(mg / mL) Max Solubility | 50 |
DMSO(mM) Max Solubility | 93.5436193897214 |
Water(mg / mL) Max Solubility | <1 |