Dalpiciclib
Based on 2 publication(s) in Google Scholar
Dalpiciclib (SHR-6390) is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4 nM and 9.9 nM, respectively. Dalpiciclib shows antitumor activity against breast cancer and esophageal squamous cell carcinoma.
For research use only. We do not sell to patients.
- Purity: 99.37%
- CAS No.: 1637781-04-4
- Formula: C25H30N6O2
- Molecular Weight:446.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Dalpiciclib
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Biological Activity
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CDK4 12.4 nM (IC50) |
CDK6 9.9 nM (IC50) |
Dalpiciclib (0-4 μM, 72 h) inhibits cell proliferation in a dose-dependent manner[3].
Dalpiciclib (0-10 μM, 6 d) inhibits the proliferation of retinoblastoma-positive tumor cell lines[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Eca 109, Eca 9706, and KYSE-510 ESCC cell lines
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Concentration:0-4 μM
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Incubation Time:72 hours
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Result:Inhibited cell proliferation in a dose-dependent manner, with Eca 109 being the relative sensitive one and Eca 9706 being the relative resistant one.
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Cell Line:MCF7, MCF7/TR, BT-474/T cell lines
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Concentration:0-10 μM
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Incubation Time:6 days
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Result:Inhibited MCF7/TR cells, parental MCF7 cells and BT-474/T resistant cells with the IC50 values of 229.5, 115.4 and 210.7 nM, respectively.
Dalpiciclib combined with Paclitaxel (PTX) or Cisplatin (CDDP) offer synergistic inhibitory effects in ESCC xenografts[3].
Dalpiciclib (oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days) shows antitumor activity in human xenograft models [4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID mice (ESCC PDXs models) [3]
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Dosage:150 mg/kg
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Administration:Oral gavage; 150 mg/kg; once weekly; 3 weeks
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Result:Suppressed the growth of tumor.
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Animal Model:5-week-old female Balb/cA-nude mice subcutaneously inoculated MCF7/ARO, COLO 205 and U87MG[4]
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Dosage:37.5 mg/kg, 75 mg/kg, 150 mg/kg
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Administration:Oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days
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Result:Caused regression of all tumor xenografts at the highest dose tested.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1637781-04-4
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Appearance Solid
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Molecular Weight 446.54
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Formula C25H30N6O2
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Color Off-white to light yellow
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SMILES
O=C1C(C(C)=O)=C(C)C2=C(N1C3CCCC3)N=C(NC4=NC=C(C5CCNCC5)C=C4)N=C2
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Synonyms
SHR-6390
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 50 mg/mL (111.97 mM; ultrasonic and warming and adjust pH to 7 with 1 M HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
1 M HCl : 5 mg/mL (11.20 mM; ultrasonic and warming and heat to 60°C)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (5.60 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (5.60 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Jose Manuel Perez-Garcia, et al. Perez-Garcia JM, Cortes J, Llombart-Cussac A. CDK4/6 inhibitors in breast cancer: spotting the difference. Nat Med. 2021 Nov;27(11):1868-1869. [Content Brief]
[2]. Pin Zhang, et al. A phase 1 study of dalpiciclib, a cyclin-dependent kinase 4/6 inhibitor in Chinese patients with advanced breast cancer. Biomark Res. 2021 Apr 12;9(1):24. [Content Brief]
[3]. Jiayuan Wang, et al. CDK4/6 inhibitor-SHR6390 exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated Rb and inducing G1 cell cycle arrest. J Transl Med. 2017 Jun 2;15(1):127. [Content Brief]
[4]. Fei Long, et al. Preclinical characterization of SHR6390, a novel CDK 4/6 inhibitor, in vitro and in human tumor xenograft models. Cancer Sci. 2019 Apr;110(4):1420-1430. [Content Brief]
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. 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 |
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| 1 M HCl / DMSO | 1 mM | 2.2394 mL | 11.1972 mL | 22.3944 mL | 55.9860 mL |
| 5 mM | 0.4479 mL | 2.2394 mL | 4.4789 mL | 11.1972 mL | |
| 10 mM | 0.2239 mL | 1.1197 mL | 2.2394 mL | 5.5986 mL | |
| DMSO | 15 mM | 0.1493 mL | 0.7465 mL | 1.4930 mL | 3.7324 mL |
| 20 mM | 0.1120 mL | 0.5599 mL | 1.1197 mL | 2.7993 mL | |
| 25 mM | 0.0896 mL | 0.4479 mL | 0.8958 mL | 2.2394 mL | |
| 30 mM | 0.0746 mL | 0.3732 mL | 0.7465 mL | 1.8662 mL | |
| 40 mM | 0.0560 mL | 0.2799 mL | 0.5599 mL | 1.3997 mL | |
| 50 mM | 0.0448 mL | 0.2239 mL | 0.4479 mL | 1.1197 mL | |
| 60 mM | 0.0373 mL | 0.1866 mL | 0.3732 mL | 0.9331 mL | |
| 80 mM | 0.0280 mL | 0.1400 mL | 0.2799 mL | 0.6998 mL | |
| 100 mM | 0.0224 mL | 0.1120 mL | 0.2239 mL | 0.5599 mL |
Dalpiciclib Related Classifications
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