Trilaciclib hydrochloride
Based on 1 publication(s) in Google Scholar
Trilaciclib (G1T28) hydrochloride is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib hydrochloride attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy.
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- Purity: 99.69%
- CAS No.: 1977495-97-8
- 화학식: C24H32Cl2N8O
- 분자량:519.47
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Trilaciclib hydrochloride
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Biological Activity
제품 설명
IC50 & Target
[1]|
Cdk4/cyclin D1 1 nM (IC50) |
cdk6/cyclin D3 4 nM (IC50) |
In Vitro
Trilaciclib hydrochloride (10-1000 nM; 24 h) reversibly modulates the proliferation of mouse and canine bone marrow hematopoietic stem and progenitor cells[1].
Trilaciclib hydrochloride (10-1000 nM; 24 h) can arrest the cell cycle of CDK4/6-dependent cells in the G1 phase, with an EC50 of 30 nM for HS68[1].
Trilaciclib hydrochloride (300 nM; 16 or 48 h) protects CDK4/6 dependent cells (HS68, WM2664) from chemotherapy-induced damage, and attenuates chemotherapy-induced-apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HS68, WM2664 cells
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Concentration:300 nM
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Incubation Time:8h for measure γH2AX foci (DNA damage); 48 hours to measure caspase 3/7 activity (apoptosis).
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Result:Elicited a robust dose-dependent decrease in caspase 3/7 activation suggesting an attenuation of apoptosis.
Resulted a dose-dependent decrease in γH2AX foci in all DNA damaging chemotherapies tested (carboplatin, doxorubicin, etoposide, camptothecin).
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Cell Line:HS68, WM2664 cells
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Concentration:10, 30, 100, 300, 1000 nM
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Incubation Time:24 h
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Result:Inhibited only CDK4/6-dependent cells, with EC50 of 30 nM for HS68 cell.
Singnificantly decreased the S phase cell numbers, increased the G1 phase cell numbers.
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Cell Line:HS68, WM2664 cells
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Concentration:10, 30, 100, 300, 1000 nM
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Incubation Time:16 h
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Result:Blocked RB phosphorylation in the RB dependent cell lines by 16 hours post exposure, while the CDK4/6-independent cell line (A2058) exhibits no RB or pRB expression. Suggesting an attenuation of chemotherapy-induced DNA damag
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:FVB/n female C57Bl6 mice[1]
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Dosage:50, 100, 150 mg/kg
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Administration:Po; single dose; treated followed 11 or 23 hours later by a single injection of EdU (HY-118411) (100 μg; ip); mouse were euthanized 1 hour after EdU injection.
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Result:Showed a dose-dependent decrease in caspase 3/7 activation.
Attenuated chemotherapy-induced myelosuppression in mice.
Chemical Information
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CAS No. 1977495-97-8
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Appearance Solid
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분자량 519.47
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화학식 C24H32Cl2N8O
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Color Light yellow to yellow
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SMILES
O=C1C2=CC3=CN=C(NC4=CC=C(N5CCN(C)CC5)C=N4)N=C3N2C6(CCCCC6)CN1.[H]Cl.[H]Cl
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Synonyms
G1T28 hydrochloride
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
용액&용해도
In Vitro:
H2O : 10 mg/mL (19.25 mM; Need ultrasonic)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.9250 mL | 9.6252 mL | 19.2504 mL | 48.1260 mL |
| 5 mM | 0.3850 mL | 1.9250 mL | 3.8501 mL | 9.6252 mL | |
| 10 mM | 0.1925 mL | 0.9625 mL | 1.9250 mL | 4.8126 mL | |
| 15 mM | 0.1283 mL | 0.6417 mL | 1.2834 mL | 3.2084 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Trilaciclib hydrochloride Related Classifications
HY-101467A Related Classifications
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