Atuveciclib Racemate
Based on 1 publication(s) in Google Scholar
Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib. Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.34%
- CAS No.: 1414943-88-6
- Formule: C18H18FN5O2S
- Masse moléculaire:387.43
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Atuveciclib Racemate
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Activité biologique
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CDK9 |
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Cell Line
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Type | Value | Description | References |
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| A2780 | IC50 |
380 nM
Compound: Atuveciclib
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Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth in presence of fetal calf serum incubated for 96 hrs measured by celltiter-glo luminescent cell viability assay
Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth in presence of fetal calf serum incubated for 96 hrs measured by celltiter-glo luminescent cell viability assay
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[PMID: 34264057] |
| A549 | IC50 |
3.29 μM
Compound: BAY-1143572
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Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
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[PMID: 33338869] |
| B16 | IC50 |
1.47 μM
Compound: BAY-1143572
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Antiproliferative activity against mouse B16 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against mouse B16 cells incubated for 72 hrs by MTT assay
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[PMID: 33338869] |
| HCT-116 | IC50 |
2.94 μM
Compound: BAY-1143572
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Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay
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[PMID: 33338869] |
| HepG2 | IC50 |
2.7 μM
Compound: BAY-1143572
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Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay
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[PMID: 33338869] |
| MCF7 | IC50 |
5.52 μM
Compound: BAY-1143572
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Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
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[PMID: 33338869] |
| MOLM-13 | IC50 |
0.2 μM
Compound: BAY-1143572
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Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by MTT assay
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[PMID: 33338869] |
| MOLM-13 | IC50 |
310 nM
Compound: Atuveciclib
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Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth in presence of fetal calf serum incubated for 96 hrs measured by celltiter-glo luminescent cell viability assay
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth in presence of fetal calf serum incubated for 96 hrs measured by celltiter-glo luminescent cell viability assay
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[PMID: 34264057] |
| MV4-11 | IC50 |
0.56 μM
Compound: BAY-1143572
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Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by MTT assay
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[PMID: 33338869] |
Atuveciclib (BAY-1143572) inhibits the proliferation of 7 MLL-rearrangements positive and negative AML cell lines with a median IC50 of 385 nM (range 230-1100 nM) and induces apoptosis[1]. Atuveciclib (BAY-1143572) has potent and highly selective PTEFb-kinase inhibitory activity in the low nanomolar range against PTEFb/CDK9 and an at least 50-fold selectivity against other CDKs. Atuveciclib (BAY-1143572) shows a favorable selectivity against a panel of non-CDK kinases. It shows broad antiproliferative activity against a panel of tumor cell lines with sub-micromolar IC50 values. The concentration-dependent inhibition of the phosphorylation of the RNA polymerase II and downstream reduction of MYC mRNA and protein levels is observed[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1414943-88-6
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Appearance Solid
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Masse moléculaire 387.43
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Formule C18H18FN5O2S
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Color White to off-white
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SMILES
N=S(CC1=CC(NC2=NC(C3=CC=C(F)C=C3OC)=NC=N2)=CC=C1)(C)=O
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Synonyms
BAY-1143572 Racemate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Haematologica
Setd2 regulates quiescence and differentiation of adult hematopoietic stem cells by restricting RNA polymerase II elongation. [Abstract]2018 Jul;103(7):1110-1123. PMID: 29650642
Atuveciclib Racemate purchased from MedChemExpress. Usage Cited in: Haematologica. 2018 Jul;103(7):1110-1123. [Abstract]
Treat c-Kit+ BM cells from Setd2f/f/Vav1-Cre mice with JQ1 500nM, EPZ-5676 1uM, BAY 1143572 400nM for 24 hours. Then cells are collected to determined the proteins levels of H3K36me1/2, H3K4me3, H3K79me2, H3K27me3, H3, RNA pol II (Ser2P), pol II (Ser5P), Gata1, Gata3, Myc, and β-actin by immunoblotting.
Solvant et solubilité
DMSO : 100 mg/mL (258.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5811 mL | 12.9056 mL | 25.8111 mL | 64.5278 mL |
| 5 mM | 0.5162 mL | 2.5811 mL | 5.1622 mL | 12.9056 mL | |
| 10 mM | 0.2581 mL | 1.2906 mL | 2.5811 mL | 6.4528 mL | |
| 15 mM | 0.1721 mL | 0.8604 mL | 1.7207 mL | 4.3019 mL | |
| 20 mM | 0.1291 mL | 0.6453 mL | 1.2906 mL | 3.2264 mL | |
| 25 mM | 0.1032 mL | 0.5162 mL | 1.0324 mL | 2.5811 mL | |
| 30 mM | 0.0860 mL | 0.4302 mL | 0.8604 mL | 2.1509 mL | |
| 40 mM | 0.0645 mL | 0.3226 mL | 0.6453 mL | 1.6132 mL | |
| 50 mM | 0.0516 mL | 0.2581 mL | 0.5162 mL | 1.2906 mL | |
| 60 mM | 0.0430 mL | 0.2151 mL | 0.4302 mL | 1.0755 mL | |
| 80 mM | 0.0323 mL | 0.1613 mL | 0.3226 mL | 0.8066 mL | |
| 100 mM | 0.0258 mL | 0.1291 mL | 0.2581 mL | 0.6453 mL |
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