| Size | Price | Stock | Qty |
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| 10mg |
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CDK4/6/1 Inhibitor is a novel and potent CDK4/6 inhibitor ( IC50s = 3 and 1 nM) with anticancer effects. It exhibits high anti-proliferative activity by arresting U87MG cells in G1 phase.
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| ln Vitro |
Crozbaciclib is an effective anti-proliferative drug that only arrests U87MG cells in G1 (IC50=15.3 ± 2.9 nM in the anti-proliferation experiment). Crozbaciclib (13.72 nM; 24 h) significantly increased the proportion of G1 cells in U87MG cells[1].
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| ln Vivo |
An orthotopic xenograft mouse model of glioblastoma multiforme displays tumor growth suppression values ranging from 62% to 99% when treated with crozbaciclib (3.125-50 mg/kg). Moreover, Crozbaciclib causes a negligible reduction in body weight. At a dosage of 50 mg/kg, crozbaciclib significantly extends life duration in mice, as evidenced by the median survival time of animals treated with a vehicle increasing by 162%[1].
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| Cell Assay |
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| References |
[1]. Yin L, et al. A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy. Eur J Med Chem. 2018 Jan 20;144:1-28
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| Molecular Formula |
C28H30F2N6
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|---|---|
| Molecular Weight |
488.57
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| Exact Mass |
488.25
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| CAS # |
2099128-41-1
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| Related CAS # |
Crozbaciclib fumarate;2567494-39-5
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| PubChem CID |
129202507
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| Appearance |
Off-white to yellow solid
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| LogP |
4.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
36
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| Complexity |
795
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C1(CCCC1)C2=CC(C3=NC(NC4=CC=C(C5CCN(C)CC5)C=N4)=NC=C3F)=C6)=NC2=C6F
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| InChi Key |
AEFFENQISAXIKE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H30F2N6/c1-17-28(9-3-4-10-28)21-13-20(14-22(29)26(21)33-17)25-23(30)16-32-27(35-25)34-24-6-5-19(15-31-24)18-7-11-36(2)12-8-18/h5-6,13-16,18H,3-4,7-12H2,1-2H3,(H,31,32,34,35)
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| Chemical Name |
5-fluoro-4-(7'-fluoro-2'-methylspiro[cyclopentane-1,3'-indole]-5'-yl)-N-[5-(1-methylpiperidin-4-yl)pyridin-2-yl]pyrimidin-2-amine
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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) |
DMSO: ~33.3 mg/mL (~68.2 mM; with ultrasonication and adjustment of pH to 3 with 1 M HCl)
1 M HCl: ~25 mg/mL (~51.2 mM; with ultrasonication) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0468 mL | 10.2339 mL | 20.4679 mL | |
| 5 mM | 0.4094 mL | 2.0468 mL | 4.0936 mL | |
| 10 mM | 0.2047 mL | 1.0234 mL | 2.0468 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.
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