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Chemical Structure| 210829-30-4 Chemical Structure| 210829-30-4

Structure of Gemcitabine elaidate
CAS No.: 210829-30-4

Chemical Structure| 210829-30-4

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Gemcitabine elaidate (CP-4126) is a lipophilic prodrug of Gemcitabine. It undergoes conversion to Gemcitabine by esterases prior to phosphorylation. Gemcitabine elaidate demonstrates anti-tumor activity.

Synonyms: CO-101; Cp-4126; Gemcitabine 5'-elaidate

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Product Details of Gemcitabine elaidate

CAS No. :210829-30-4
Formula : C27H43F2N3O5
M.W : 527.64
SMILES Code : O[C@@H](C(F)(F)[C@H](N1C(N=C(C=C1)N)=O)O2)[C@H]2COC(CCCCCCC/C=C/CCCCCCCC)=O
Synonyms :
CO-101; Cp-4126; Gemcitabine 5'-elaidate
MDL No. :MFCD15145214

Safety of Gemcitabine elaidate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H361
Precautionary Statements:P501-P202-P201-P264-P280-P302+P352-P308+P313-P337+P313-P305+P351+P338-P362+P364-P332+P313-P405

Related Pathways of Gemcitabine elaidate

DNA

Isoform Comparison

Biological Activity

Description
Gemcitabine elaidate (CP-4126) is a lipophilic prodrug of Gemcitabine. It undergoes conversion to Gemcitabine by esterases prior to phosphorylation. Gemcitabine elaidate demonstrates anti-tumor activity [1][2].

In Vitro:

Cell Line
Concentration Treated Time Description References
MB49 8×10^−6M 2 hours Evaluate the in vitro therapeutic efficacy of targeted photodynamic-chemotherapy, showing that 50GCG significantly increased cytotoxicity after light irradiation. Adv Sci (Weinh). 2022 May;9(16):e2200731
UMUC3 8×10^−6M 2 hours Evaluate the in vitro therapeutic efficacy of targeted photodynamic-chemotherapy, showing that 50GCG significantly increased cytotoxicity after light irradiation. Adv Sci (Weinh). 2022 May;9(16):e2200731
MIA PaCa-2 cells 1.0 ± 0.2 µM 48 hours Evaluate the cytotoxicity of L_GEM on MIA PaCa-2 cells, results showed that L_GEM had significantly higher cytotoxicity than GEM. Cell Death Discov. 2024 Mar 29;10(1):158
MIA PaCa-2 cells 200 nM 72 hours Evaluate the cytotoxic effect of L_GEM combined with ONC201, results showed that the combination treatment significantly enhanced cytotoxicity. Res Sq [Preprint]. 2023 Jul 11:rs

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Orthotopic bladder cancer model Intravesical delivery 8×10^−6M Once weekly for a total of four doses Evaluate the in vivo therapeutic efficacy of targeted photodynamic-chemotherapy, showing that 50GCG combined with wireless LED light significantly reduced tumor burden. Adv Sci (Weinh). 2022 May;9(16):e2200731
Mice KPC triple mutant xenograft tumor-bearing mice Systemic administration 20 mg/kg (L_GEM), 15 mg/kg (ONC201) Once a week, for 11 days Evaluate the inhibitory effect of L_GEM combined with ONC201 on tumor growth in KPC mice, results showed significant tumor growth inhibition. Cell Death Discov. 2024 Mar 29;10(1):158
Mice KPC triple mutant xenograft tumor model 20 mg/kg Evaluate the anti-tumor effect of L_GEM combined with ONC201 in vivo, results showed that the combination treatment significantly inhibited tumor growth. Res Sq [Preprint]. 2023 Jul 11:rs

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.48mL

1.90mL

0.95mL

18.95mL

3.79mL

1.90mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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