1. Cell Cycle/DNA Damage
  2. CDK

BAY-1143572 

Cat. No.: HY-12871B Purity: 99.42% ee.: 99.10%
Handling Instructions

BAY-1143572 is a potent and highly selective, oral PTEFb/CDK9 inhibitor. BAY-1143572 inhibits CDK9/CycT1 with an IC50 of 13 nM.

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

BAY-1143572 Chemical Structure

BAY-1143572 Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Other Forms of BAY-1143572:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BAY-1143572 is a potent and highly selective, oral PTEFb/CDK9 inhibitor. BAY-1143572 inhibits CDK9/CycT1 with an IC50 of 13 nM.

IC50 & Target[1]

CDK9/CycT1

13 nM (IC50)

CDK9/CycT1(h)

6 nM (IC50)

CDK3/CycE(h)

890 nM (IC50)

CDK2/CycE(h)

1000 nM (IC50)

CDK1/CycB(h)

1100 nM (IC50)

CDK5/p35(h)

1600 nM (IC50)

In Vitro

Positive transcription elongation factor b (PTEFb) is a heterodimer of CDK9 and one of four cyclin partners, cyclin T1, cyclin K, cyclin T2a or cyclin T2b. BAY-1143572 (BAY 1143572) demonstrates potent antiproliferative activity against HeLa cells (IC50=920 nM) and MOLM-13 cells (IC50=310 nM)[1].

In Vivo

In vivo efficacy studies in the MOLM-13 xenograft model in mice, BAY-1143572 (BAY 1143572) demonstrates great potency and high antitumor efficacy. Daily administration of BAY-1143572 at 6.25 or 12.5 mg/kg results in a dose-dependent antitumor efficacy with a treatment-to-control (T/C) ratio of 0.64 and 0.49, respectively (p<0.001). In a separate experiment with a higher daily dose of 20 or 25 mg/kg BAY-1143572, antitumor efficacy with a T/C ratio of 0.41 and 0.31, respectively, is observed (p<0.001). The 25 mg/kg once daily dose is the maximum tolerated dose in nude mice. Furthermore, BAY-1143572 administered at 25 or 35 mg/kg, three days on / two days off, results in a T/C ratio of 0.33 and 0.20, respectively (p<0.001). Treatment with BAY-1143572 is well-tolerated, as demonstrated by less than 10 % mean body weight reduction throughout the study. In an in vivo pharmacokinetic study in rats, BAY-1143572 shows low blood clearance (CLb 1.1 L/kg per hour)[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 128.5 mg/mL (331.67 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5811 mL 12.9056 mL 25.8111 mL
5 mM 0.5162 mL 2.5811 mL 5.1622 mL
10 mM 0.2581 mL 1.2906 mL 2.5811 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

HeLa human cervical tumor cells (CCL-2) and MOLM-13 human acute myeloid leukemia cells (ACC 554) are propagated under the suggested growth conditions in a humidified 37°C incubator. Proliferation assays are conducted in 96-well plates at densities of 3000 (HeLa) and 5000 (MOLM-13) cells per well in the growth medium containing 10 % fetal calf serum (FCS). Cells are treated in quadruplicate with serial dilutions of test compounds (e.g., BAY-1143572) for 96 h. Relative cell numbers are quantified by crystal violet staining (HeLa) or CellTitre-Glo Luminescent Cell Viability Assay (MOLM-13). IC50 values are determined by means of a four-parameter fit on measurement data which are normalized to vehicle (DMSO) treated cells (=100 %) and measurement readings taken immediately before compound exposure (=0 %)[1].

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

Animal Administration
[1]

Mice and Rats[1]
For the acute myeloid leukemia (AML) mouse model, 2×106 MOLM-13 human AML cells are inoculated subcutaneously to the left flank of female NMRI nu/nu mice (18-21 g, 5-6 weeks). For the AML model in rats, 2×106 MV4-11 human AML cells are inoculated subcutaneously to the left flank of female athymic nude rats (160-200 g, 5-6 weeks). Animals are stratified into treatment and control groups (n=8-13/group for mice, n=12/group for rats) based on primary tumor size. Treatments are started 3-13 days after tumor cell inoculation when the average tumor sizes are 23-38 mm2 and 43 mm2 for mice and rats, respectively. The 20 and 25 mg/kg once daily dose is for nude mice. Furthermore, BAY-1143572 administered at 25 or 35 mg/kg, three days on/two days off. BAY-1143572 is administered daily oral administration of BAY-1143572 at 12 mg/kg for rats. Unless otherwise indicated, all treatments are administered orally (p.o.) and are continued until the end of the experiment. Body weight and tumor areas (longest diameter multiplied by its perpendicular) measured by caliper are determined at least twice weekly. T/C ratios are calculated by dividing the mean tumor area of the treatment group by the mean tumor area of the vehicle group at the time point when the vehicle group is sacrificed[1].

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

References
Molecular Weight

387.43

Formula

C₁₈H₁₈FN₅O₂S

SMILES

N=[[email protected]](CC1=CC(NC2=NC(C3=CC=C(F)C=C3OC)=NC=N2)=CC=C1)(C)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
BAY-1143572
Cat. No.:
HY-12871B
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BAY-1143572

Cat. No.: HY-12871B