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Cat. No.: HY-182360

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Cytisine-platinum(IV) prodrug-1

Cytisine-Platinum(IV) Prodrug-1 is a Pt(IV) prodrug incorporating the natural compound Cytisine (HY-N0175) with antiproliferative activity against tumor cells. Cytisine-Platinum(IV) Prodrug-1 promotes calcium transfer across the IP3R1-GRP75-VDAC1 axis to drive mitochondrial calcium overload. Cytisine-Platinum(IV) Prodrug-1 initiates unfolded protein response via PERK, eIF2α, ATF4, and CHOP to modulate Bcl-2 and Bax, triggering apoptosis. Cytisine-Platinum(IV) Prodrug-1 induces mitochondrial dysfunction, ROS production, reduced ATP synthesis, DNA damage, and S-phase cell cycle arrest. Cytisine-Platinum(IV) Prodrug-1 activates the cGAS-STING pathway, reduces PD-L1 expression, drives immunogenic cell death. Cytisine-Platinum(IV) Prodrug-1 exhibits high physiological stability, efficient cellular accumulation, and enhanced platinum-DNA binding, and inhibits tumor growth in mouse models with reduced systemic toxicity. Cytisine-Platinum(IV) Prodrug-1 can be used for the research of lung cancer.

For research use only. We do not sell to patients.

Formula: C₂₉H₅₁Cl₂N₅O₆Pt
Molecular Weight:831.74

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Cytisine-platinum(IV) prodrug-1 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

eIF2

Bcl-2

Bax

All Bcl-2 Family Isoforms :

All DNA/RNA Synthesis Isoforms :

In Vitro

Cytisine-Platinum(IV) Prodrug-1 (Compound CP12) (72 h) potently inhibits the viability of H226, SW1990, HepG2, and MDA-MB-231 tumor cells with IC₅₀ values of 0.09, 0.15, 0.21, and 0.61 μM, while showing high selectivity for tumor cells over normal PUMC-HUVEC-T1 cells^[1].
Cytisine-Platinum(IV) Prodrug-1 (100 μM; 12-72 h) exhibits high stability in PBS, RPMI-1640 medium, and rat plasma when incubated at 37 °C^[1].
Cytisine-Platinum(IV) Prodrug-1 (100 μM; 16 h) undergoes intracellular reductive activation in H226 cells, releasing the cytisine derivative CYT-COOH^[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 24 h) potently inhibits colony formation in H226 cells and effectively kills H₂26 cells^[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 24 h) potently inhibits the migration and apoptosis of H226 cells^[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 12 h) induces strong S-phase cell cycle arrest in H226 cells, with 62.19% of cells accumulating in S phase, and reduces cyclin D1 expression^[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 24 h) induces endoplasmic reticulum stress in H226 cells, activates the IP₃R1-GRP75-VDAC1 axis, and causes mitochondrial calcium overload, which contributes to its antitumor activity^[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 24 h) induces mitochondrial dysfunction in H226 cells, characterized by reduced ATP production, MMP collapse, increased ROS generation, cytochrome C release, and disrupted mitochondrial morphology^[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 24 h) activates the cGAS-STING pathway in H226 cells, upregulating key pathway proteins and promoting IL-6 secretion^[1].
Cytisine-Platinum(IV) Prodrug-1 (1 μM; 24 h) potently induces immunogenic cell death in H226 cells, characterized by increased CRT exposure, HMGB1, LDH, and ATP release, and reduced PD-L1 expression^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Migration Assay ^[1]

Cell Line:

H226
Concentration:

1 μM
Incubation Time:

24 h
Result:

Drastically suppressed H226 cell migration, resulting in a wound healing rate of only 2.44%.

Apoptosis Analysis^[1]

Cell Line:

H226
Concentration:

1 μM
Incubation Time:

24 h
Result:

Induced a high rate of apoptosis in H226 cells, with an apoptosis rate of 80.4%.

Cell Cycle Analysis^[1]

Cell Line:

H226
Concentration:

1 μM
Incubation Time:

12 h
Result:

Resulted in significant S-phase cell cycle arrest in H226 cells, with 62.19% of cells in S phase, and complete blockage of transition from S to G2 phase.
Reduced cyclin D1 protein expression.

Western Blot Analysis^[1]

Cell Line:

H226
Concentration:

1 μM
Incubation Time:

24 h
Result:

Significantly upregulated protein expression of p-PERK, p-eIF2α, ATF4, and CHOP, while downregulating Bcl-2 and upregulating Bax.
Upregulated expression of IP3R1, GRP75, and VDAC1, key components of the ER-mitochondria calcium transfer axis.
Resulted in a significant increase in both cytosolic and mitochondrial Ca²⁺ levels.
Pretreatment with 2-APB reduced Ca²⁺ accumulation in the cytosol and mitochondria, and partially reversed CP12-induced cytotoxicity.

Western Blot Analysis^[1]

Cell Line:

H226
Concentration:

1 μM
Incubation Time:

24 h
Result:

Significantly upregulated protein expression of cGAS, p-STING, p-IRF3, and p-TBK1, indicating activation of the cGAS-STING pathway.
Induced the highest level of IL-6 secretion among tested compounds, with levels 2.14-fold higher than those induced by CDDP.

Immunofluorescence^[1]

Cell Line:

H226
Concentration:

1 μM
Incubation Time:

24 h
Result:

Significantly increased CRT surface exposure and HMGB1 release, and reduced PD-L1 protein expression in H226 cells.

In Vivo

Cytisine-Platinum(IV) Prodrug-1 (Compound CP12) (2-4 mg/kg Pt; i.v.; once every 3 days; 6 total doses) potently inhibits H226 lung cancer tumor growth in nude mice, with no significant hepatorenal toxicity and minimal body weight impact^[1].
Cytisine-Platinum(IV) Prodrug-1 (2-4 mg/kg Pt; i.v.; once every 3 days; 6 total doses) potently inhibits LLC lung cancer tumor growth in immunocompetent mice, while activating the cGAS-STING pathway, inducing immunogenic cell death, and enhancing cytotoxic T-cell infiltration to remodel the tumor microenvironment^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nude (male, 4-6 weeks old, 18 g, H226 cell-derived xenograft model)^[1]
Dosage:

2, 4 mg/kg Pt
Administration:

i.v.; once every 3 days; 6 total doses
Result:

Achieved a tumor growth inhibition (TGI) rate of 59.3%.
Achieved a tumor growth inhibition (TGI) rate of 72.7%.
Showed no significant body weight loss, with the low-dose group having body weight comparable to the control group, and the high-dose group showing an increasing body weight trend.
Caused no remarkable abnormalities in liver, lung, or kidney tissue.
Achieved significantly higher platinum accumulation in tumor tissue and lower platinum accumulation in renal tissue compared to CDDP (HY-17394).
Induced a concentration-dependent increase in necrotic area in tumor tissue.

Animal Model:

C57BL/6 (male, 5 weeks old, 18 g, LLC cell-derived xenograft model)^[1]
Dosage:

2, 4 mg/kg Pt
Administration:

i.v.; once every 3 days; 6 total doses
Result:

Achieved a tumor growth inhibition (TGI) rate of 69.1%.
Achieved a tumor growth inhibition (TGI) rate of 81.1%.
Showed no significant body weight loss.
Potently activated the cGAS-STING pathway in tumor tissue in a dose-dependent manner.
Significantly increased calreticulin (CRT) exposure and high mobility group box 1 (HMGB1) release in tumor tissue.
Substantially increased infiltration of CD3⁺ and CD8⁺ T cells in tumors compared to control and CDDP groups.

Chemical Information

Molecular Weight 831.74
Formula C₂₉H₅₁Cl₂N₅O₆Pt
SMILES

[NH3][Pt](Cl)(Cl)([NH3])(OC(CCCC(N1C[C@](C2=CC=CC(N2C[C@@]3(C1)[H])=O)(C3)[H])=O)=O)OC(NCCCCCCCCCCCC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Sang RX, et al. Antitumor Cytisine-Platinum(IV) Prodrugs Potentiate Crosstalk between Endoplasmic Reticulum and Mitochondria through Calcium Overload Accompanied by Immunogenic Cell Death. J Med Chem. 2026;69(7):8148-8167. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Cytisine-platinum(IV) prodrug-1

All Bcl-2 Family Isoforms

All DNA/RNA Synthesis Isoforms