| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| References | |
|---|---|
| Additional Infomation |
Dalpiciclib isethionate is the isothiocyanate form of dalpiciclib, a highly bioavailable, orally bioavailable cyclin-dependent kinase (CDK) inhibitor with potential antitumor activity. After oral administration, dalpiciclib selectively inhibits cyclin-dependent kinases 4 (CDK4) and 6 (CDK6). This inhibits phosphorylation of early G1 phase retinoblastoma (Rb) proteins, thereby preventing CDK-mediated G1-S phase transition and leading to cell cycle arrest. This inhibits DNA replication and reduces tumor cell proliferation. CDK4 and 6 are serine/threonine kinases upregulated in various tumor cell types and play a crucial role in the regulation of cell cycle progression.
|
| Molecular Formula |
C27H36N6O6S
|
|---|---|
| Molecular Weight |
572.68
|
| Exact Mass |
572.242
|
| CAS # |
1980822-14-7
|
| Related CAS # |
Dalpiciclib; 1637781-04-4
|
| PubChem CID |
132211171
|
| Appearance |
Typically exists as solids at room temperature
|
| Hydrogen Bond Donor Count |
4
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
40
|
| Complexity |
890
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)C4CCNCC4)C5CCCC5)C(=O)C.C(CS(=O)(=O)O)O
|
| InChi Key |
IWHGWNIWQZCOIR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H30N6O2.C2H6O4S/c1-15-20-14-28-25(29-21-8-7-18(13-27-21)17-9-11-26-12-10-17)30-23(20)31(19-5-3-4-6-19)24(33)22(15)16(2)32;3-1-2-7(4,5)6/h7-8,13-14,17,19,26H,3-6,9-12H2,1-2H3,(H,27,28,29,30);3H,1-2H2,(H,4,5,6)
|
| Chemical Name |
6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperidin-4-yl-2-pyridinyl)amino]pyrido[2,3-d]pyrimidin-7-one;2-hydroxyethanesulfonic acid
|
| Synonyms |
SHR-6390 isethionate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7462 mL | 8.7309 mL | 17.4618 mL | |
| 5 mM | 0.3492 mL | 1.7462 mL | 3.4924 mL | |
| 10 mM | 0.1746 mL | 0.8731 mL | 1.7462 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT07238881
Conditions:Hepatocellulcar CarcinomaLink: https://clinicaltrials.gov/ct2/show/NCT07189884
Conditions:Locally Advanced Breast Cancer (LABC)Link: https://clinicaltrials.gov/ct2/show/NCT06208410
Conditions:Advanced Solid Tumors
Title:Treatment of Dalpiciclib Combined With Pyrotinib for Trastuzumab-sensitive HER2+ Advanced Breast Cancer(DAP-Her-02)
Status:Unknown status
updateDate:2023-09-25
Ctid:NCT05328440
Link: https://clinicaltrials.gov/ct2/show/NCT05328440
Conditions:Breast NeoplasmsProducts are for research use only; We do not sell to patients
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