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Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable, and comparable potency inhibitor of CDK4 and CKD6 with IC50s of 12.4 nM and 9.9 nM, respectively. Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $152 | In Stock | In Stock | |
| 5 mg | $378 | In Stock | In Stock | |
| 10 mg | $592 | In Stock | In Stock | |
| 25 mg | $1,190 | In Stock | In Stock | |
| 50 mg | $1,950 | In Stock | In Stock | |
| 100 mg | $2,630 | In Stock | In Stock |
| Description | Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable, and comparable potency inhibitor of CDK4 and CKD6 with IC50s of 12.4 nM and 9.9 nM, respectively. Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest. |
| Targets&IC50 | CDK6:9.9 nM, CDK4:12.4 nM |
| In vitro | Dalpiciclib inhibits cell proliferation in a dose-dependent manner following administration of 0-4 μM for 72?hours[2].In the relative sensitive Eca 109 and KYSE-510 cell lines, Dalpiciclib significantly blocks Rb phosphorylation at serine 780 after 24 hours of administration and induces cell cycle arrest but not in relative resistant Eca 9706 cell line[2]. |
| In vivo | Dalpiciclib administered at 150 mg/kg weekly for 3 weeks by oral gavage has antitumor activity in ESCC xenografts[2]. Dalpiciclib in combination with Paclitaxel or Cisplatin provides synergistic inhibition in ESCC xenografts[2]. |
| Synonyms | SHR-6390 |
| Molecular Weight | 446.54 |
| Formula | C25H30N6O2 |
| Cas No. | 1637781-04-4 |
| Smiles | O=C1N(C=2C(C(C)=C1C(C)=O)=CN=C(NC3=CC=C(C=N3)C4CCNCC4)N2)C5CCCC5 |
| Relative Density. | 1.277 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||
| Solubility Information | DMSO: < 1 mg/mL (insoluble) Methanol: 1.67 mg/mL (3.74 mM), Sonication and heating to 60°C are recommended. 1M HCl: < 1 mg/mL (insoluble) | ||||||||||
Solution Preparation Table | |||||||||||
Methanol
| |||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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