(rel)-MC180295 (Synonyms: (rel)-MC180295) |
Catalog No.GC34124 |
(rel)-MC180295 ((rel)-(rel)-MC180295) es un inhibidor potente y selectivo de CDK9-Cyclin T1, con una IC50 de 5 nM, al menos 22 veces mÁs selectivo para CDK9 que para otras CDK. (rel)-MC180295 también inhibe GSK-3α y GSK-3β. (rel)-MC180295 ((rel)-(rel)-MC180295) tiene un potente efecto antitumoral.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2237942-08-2
Sample solution is provided at 25 µL, 10mM.
(rel)-MC180295 is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. (rel)-MC180295 also inhibits GSK-3α and GSK-3β. (rel)-MC180295 has potent anti-tumor effect[1].
(rel)-MC180295 (MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs, such as CDK1-Cyclin B (IC50, 138 nM), CDK2-Cyclin A (IC50, 233 nM), CDK2-Cyclin E (IC50, 367 nM), CDK3-Cyclin E (IC50, 399 nM), CDK4-Cyclin D (IC50, 112 nM), CDK5-P35 (IC50, 159 nM), CDK5-P25 (IC50, 186 nM), CDK6-Cyclin D3 (IC50, 712 nM), and CDK7-CycH/MAT1 (IC50, 555 nM). (rel)-MC180295 also inhibits GSK-3α and GSK-3β[1].(rel)-MC180295 (500 nM) reactivates epigenetically silenced genes by targeting CDK9 without affecting DNA methylation[1].(rel)-MC180295 (0.1 μM) inhibits the proliferation in cancer cells[1].
(rel)-MC180295 (MC180295; 20 mg/kg, i.p., qod) inhibits significant anti-tumor activity in mice bearing SW48 cells, shows no inhibitory activity against human T cell growth in vivo[1].
[1]. Zhang H, et al. Targeting CDK9 Reactivates Epigenetically Silenced Genes in Cancer. Cell. 2018 Nov 15;175(5):1244-1258.e26.
Cas No. | 2237942-08-2 | SDF | |
Sinónimos | (rel)-MC180295 | ||
Canonical SMILES | NC1=C(C(C2=CC=CC=C2[N+]([O-])=O)=O)SC(N[C@@H]3[C@H](C4)CC[C@H]4C3)=N1 | ||
Formula | C17H18N4O3S | M.Wt | 358.41 |
Solubility | DMSO : 100 mg/mL (279.01 mM) | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.7901 mL | 13.9505 mL | 27.901 mL |
5 mM | 0.558 mL | 2.7901 mL | 5.5802 mL |
10 mM | 0.279 mL | 1.3951 mL | 2.7901 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5
(Based on Reviews and 35 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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