BI 2536

Catalog No. A10134

BI 2536是Plk1的选择性抑制剂，可在低纳摩尔浓度下抑制Plk1酶的活性。

Product Citations

Kei K Ito, .et al. Cep57 and Cep57L1 maintain centriole engagement in interphase to ensure centriole duplication cycle, J Cell Biol, 2021, Mar 1;220(3):e202005153 PMID: 33492359
Ryuzaburo Yuki, .et al. The tyrosine kinase v-Src modifies cytotoxicities of anticancer drugs targeting cell division, J Cell Mol Med, 2021, Feb;25(3):1677-1687 PMID: 33465289
Yamagishi A, .et al. Targeting Insulin-Like Growth Factor 1 Receptor Delays M-Phase Progression and Synergizes with Aurora B Inhibition to Suppress Cell Proliferation, Int J Mol Sci, 2020, Feb 5;21(3) PMID: 32033461
Bucko PJ, .et al. Subcellular drug targeting illuminates local kinase action, Elife, 2019, Dec 24;8. pii: e52220 PMID: 31872801
Watanabe K, .et al. The Cep57-pericentrin module organizes PCM expansion and centriole engagement, Nat Commun, 2019, Feb 25;10(1):931 PMID: 30804344
Valérian Pasche, .et al. Screening a repurposing library, the Medicines for Malaria Venture Stasis Box, against Schistosoma mansoni, Parasit Vectors, 2018, 11: 298 PMID: 29764454
Takeshi Wakida, .et al. The CDK-PLK1 axis targets the DNA damage checkpoint sensor protein RAD9 to promote cell proliferation and tolerance to genotoxic stress, eLife, 2017, 6: e29953 PMID: 29254517
Majid Momeny, .et al. Dacomitinib, a pan-inhibitor of ErbB receptors, suppresses growth and invasive capacity of chemoresistant ovarian carcinoma cells, Sci Rep, 2017, 7: 4204 PMID: 28646172
Ifuji A, .et al. A novel immunofluorescence method to visualize microtubules in the antiparallel overlaps of microtubule-plus ends in the anaphase and telophase midzone, Exp Cell Res, 2017, Nov 15;360(2):347-357 PMID: 28942021

Technical details

Catalog Num	A10134
M. Wt	521.7
Formula	C28H39N7O3
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	755038-02-9
Synonyms	BI2536, BI-2536
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

Biological Activity

BI 2536是Plk1的选择性抑制剂，可在低纳摩尔浓度下抑制Plk1酶的活性。

Targets

Target	Value
PLK1	IC50: 0.83nM
PLK2	IC50: 3.5nM
PLK3	IC50: 9.0nM
PI3Kα	IC50: 2.407μM
Met	IC50: 4.754μM
Tie-2	IC50: 6.549μM
HGFR	IC50: 9.5μM
ErbB4	IC50: 9.908μM
Abl	IC50: >10μM
Axl	IC50: >10μM
AMPK	IC50: >10μM
AuroraA	IC50: >10μM
AuroraB	IC50: >10μM
βIRK	IC50: >10μM
B-Raf	IC50: >10μM
BTK	IC50: >10μM
CDK1/CyclinB1	IC50: >10μM
CDK2/CyclinE	IC50: >10μM
Chk1	IC50: >10μM
CK1	IC50: >10μM
CK2	IC50: >10μM
C-Raf	IC50: >10μM
CSK	IC50: >10μM
DYRK1A	IC50: >10μM
ECK	IC50: >10μM
ERK2	IC50: >10μM
FGFR1	IC50: >10μM
FGFR3	IC50: >10μM
FLT1	IC50: >10μM
FLT3	IC50: >10μM
GSK-3β	IC50: >10μM
Hek	IC50: >10μM
HER2	IC50: >10μM
ITK	IC50: >10μM
JAK2	IC50: >10μM
JAK3	IC50: >10μM
JNK1	IC50: >10μM
LCK	IC50: >10μM
Lyn	IC50: >10μM
MAPKAPK2	IC50: >10μM
MEK1	IC50: >10μM
MSK1	IC50: >10μM
MKK1	IC50: >10μM
NEK6	IC50: >10μM
p38α	IC50: >10μM
p38β	IC50: >10μM
p38γ	IC50: >10μM
p38δ	IC50: >10μM
PAK2	IC50: >10μM
PDGFRα	IC50: >10μM
PDGFRβ	IC50: >10μM
PDK-1	IC50: >10μM
PKA	IC50: >10μM
PKBα	IC50: >10μM
PKBβ	IC50: >10μM
PKCα	IC50: >10μM
PRAK	IC50: >10μM
RET	IC50: >10μM
ROCK2	IC50: >10μM
RON	IC50: >10μM
S6K	IC50: >10μM
SGK	IC50: >10μM
Src	IC50: >10μM
Syk	IC50: >10μM

Solubility *

In vitro (25°C)	DMSO	21 mg/mL (40.25 mM)
	Water	Insoluble
	Ethanol	98 mg/mL (187.86 mM)
In vivo	30% PEG 400+0.5% Tween 80+5% Propylene glycol	14 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	19.17 mL	95.84 mL	191.68 mL
0.5 mM	3.83 mL	19.17 mL	38.34 mL
1 mM	1.92 mL	9.58 mL	19.17 mL
5 mM	0.38 mL	1.92 mL	3.83 mL

*The above data is based on the productmolecular weight 521.7. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.