| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Ebvaciclib (PF-06873600; PF06873600) is a novel, potent, selective and orally bioavailable pan-inhibitor of cyclin-dependent kinase (CDK) with potential antitumor activity. With Ki values of 0.09 nM, 0.13 nM, and 0.16 nM, respectively, it inhibits CDK2, CDK4, and CDK6. PF-06873600 binds to CDKs specifically and inhibits their activity, exhibiting antineoplastic activity. Tumor cell proliferation is inhibited, apoptosis is induced, and cell cycle arrest results from inhibition of these kinases. Tumor cells often overexpress CDKs, ATP-dependent serine/threonine kinases that are key regulators of cell cycle progression and cellular proliferation.
| Targets |
CDK2 (Ki = 0.1 nM); CDK6 (Ki = 0.1 nM); CDK4 (Ki = 1.2 nM)
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|---|---|
| ln Vitro |
PF-06873600 is an cyclin-dependent kinase 2 (CDK2), CDK4, and CDK6 inhibitor with Ki values of 0.1, 1.2, and 0.1 nM, respectively.
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| Animal Protocol |
Mice-bearing OVCAR3 tumors
50 mg/kg p.o. |
| References | |
| Additional Infomation |
Ebvaciclib is an orally bioavailable, cyclin dependent kinase (CDK) inhibitor, with potential antineoplastic activity. Upon administration, ebvaciclib selectively targets, binds to and inhibits the activity of CDKs. Inhibition of these kinases leads to cell cycle arrest, an induction of apoptosis, and inhibition of tumor cell proliferation. CDKs are ATP-dependent serine/threonine kinases that are important regulators of cell cycle progression and proliferation and are frequently overexpressed in tumor cells.
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| Molecular Formula |
C20H27F2N5O4S
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|---|---|
| Molecular Weight |
471.521290063858
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| Exact Mass |
471.18
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| Elemental Analysis |
C, 53.99; H, 7.29; N, 13.69; O, 12.51; S, 12.53
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| CAS # |
2185857-97-8
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| Related CAS # |
PF-06873600 HCl;2185857-97-8;2185859-59-8 (SS-isomer);
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| PubChem CID |
134247638
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| Appearance |
White to light yellow solid powder
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| LogP |
1.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
859
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@]1(CCC[C@H]1N2C3=NC(=NC=C3C=C(C2=O)C(F)F)NC4CCN(CC4)S(=O)(=O)C)O
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| InChi Key |
QIEKHLDZKRQLLN-FOIQADDNSA-N
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| InChi Code |
InChI=1S/C20H27F2N5O4S/c1-20(29)7-3-4-15(20)27-17-12(10-14(16(21)22)18(27)28)11-23-19(25-17)24-13-5-8-26(9-6-13)32(2,30)31/h10-11,13,15-16,29H,3-9H2,1-2H3,(H,23,24,25)/t15-,20-/m1/s1
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| Chemical Name |
6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcyclopentyl]-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrido[2,3-d]pyrimidin-7-one
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| Synonyms |
PF06873600; Ebvaciclib; PF 06873600; PF-06873600
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| HS Tariff Code |
2934.99.9001
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| 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)
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| 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
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|---|---|
| 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 | 2.1208 mL | 10.6040 mL | 21.2080 mL | |
| 5 mM | 0.4242 mL | 2.1208 mL | 4.2416 mL | |
| 10 mM | 0.2121 mL | 1.0604 mL | 2.1208 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.
Products are for research use only; We do not sell to patients
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