Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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B129994-5mg | 5mg | In stock | $107.90 | |
B129994-10mg | 10mg | In stock | $162.90 | |
B129994-25mg | 25mg | In stock | $217.90 | |
B129994-50mg | 50mg | In stock | $271.90 | |
B129994-100mg | 100mg | In stock | $489.90 | |
B129994-250mg | 250mg | In stock | $1,102.90 | |
B129994-1g | 1g | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $3,969.90 |
Synonyms | (R)-4-(8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-ylamino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide | EN300-18167228 | (R)-4-((8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl)amino)-3-methoxy-N-(1-methylpip |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | BI 2536 treatment ranging from 10 nM to 100 nM blocks the recruitment of γ-tubulin and phosphorylation of Apc6 at mitotic centrosomes, inhibits of cohesin release from chromosome arms, and induces monopolar spindle formation and other Plk1 dependent proce |
Storage Temp | Protected from light,Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Serine/threonine-protein kinase PLK1 inhibitor |
Product Description | BI2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM. It shows 4- and 11-fold greater selectivity against Plk2 and Plk3. |
ALogP | 3.7 |
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Pubchem Sid | 488197433 |
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Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/488197433 |
IUPAC Name | 4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide |
INCHI | InChI=1S/C28H39N7O3/c1-5-22-27(37)34(3)23-17-29-28(32-25(23)35(22)20-8-6-7-9-20)31-21-11-10-18(16-24(21)38-4)26(36)30-19-12-14-33(2)15-13-19/h10-11,16-17,19-20,22H,5-9,12-15H2,1-4H3,(H,30,36)(H,29,31,32)/t22-/m1/s1 |
InChi Key | XQVVPGYIWAGRNI-JOCHJYFZSA-N |
Canonical SMILES | CCC1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C |
Isomeric SMILES | CC[C@@H]1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C |
PubChem CID | 11364421 |
Molecular Weight | 521.66 |
CAS Registry No. | 755038-02-9 |
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DiscoveRx TREEspot | BI-2536| |
PubChem CID | 11364421 |
ChEMBL Ligand | CHEMBL513909 |
ChEBI | CHEBI:49868 |
RCSB PDB Ligand | R78 |
PubChem SID | 488197433 |
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 |
---|---|---|---|
B1615031 | Certificate of Analysis | Jul 07, 2023 | B129994 |
E2309814 | Certificate of Analysis | Feb 02, 2023 | B129994 |
E2309816 | Certificate of Analysis | Feb 02, 2023 | B129994 |
E2309818 | Certificate of Analysis | Feb 02, 2023 | B129994 |
E2309820 | Certificate of Analysis | Feb 02, 2023 | B129994 |
E2309823 | Certificate of Analysis | Feb 02, 2023 | B129994 |
E2309828 | Certificate of Analysis | Feb 02, 2023 | B129994 |
E2309834 | Certificate of Analysis | Feb 02, 2023 | B129994 |
E2309837 | Certificate of Analysis | Feb 02, 2023 | B129994 |
E2309843 | Certificate of Analysis | Feb 02, 2023 | B129994 |
E2309899 | Certificate of Analysis | Feb 02, 2023 | B129994 |
L1602081 | Certificate of Analysis | Jul 11, 2022 | B129994 |
Solubility | DMSO 21 mg/mL Water <1 mg/mL Ethanol 100 mg/mL |
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Sensitivity | light sensitive |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H302:Harmful if swallowed |
Precautionary Statements | P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. |
Starting at $329.90
1. Steegmaier M, Hoffmann M, Baum A, Lénárt P, Petronczki M, Krssák M, Gürtler U, Garin-Chesa P, Lieb S, Quant J et al.. (2007) BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo.. Curr Biol, 17 (4): (316-22). [PMID:17291758] |
2. Ciceri P, Müller S, O'Mahony A, Fedorov O, Filippakopoulos P, Hunt JP, Lasater EA, Pallares G, Picaud S, Wells C et al.. (2014) Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.. Nat Chem Biol, 10 (4): (305-12). [PMID:24584101] |