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Cat. No.: HY-190596

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CyNPTi-29

CyNPTi-29 is a NAMPT inhibitor, a multi-modal small molecule obtained by covalently coupling a NAMPT inhibitor with the dye IR-808. CyNPTi-29 depletes cellular NAD, downregulates HSP90 expression, impairs mitochondrial function, and induces ROS generation and apoptosis, inhibiting tumor cell migration and colony formation. CyNPTi-29 achieves tumor cell-specific uptake and mitochondrial localization via OATP transporter mediation, and enables near-infrared fluorescence imaging and photothermal conversion for mild photothermal intervention. CyNPTi-29 inhibits tumor proliferation and lung metastasis in 4T1 breast cancer xenograft and lung metastasis mouse models. CyNPTi-29 can be used for research on breast cancer.

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

Formula: C₆₉H₇₈BrClFN₇O₅
Molecular Weight:1219.76

Storage:

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

CyNPTi-29 Chemical Structure

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Use of MCE Products

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

Biological Activity
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All HSP Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC50	0.031 μM	Antiproliferative activity against A2780 cells assessed as viability reduction incubated 72 hrs by MTT assay. Antiproliferative activity against A2780 cells assessed as viability reduction incubated 72 hrs by MTT assay.	j.ejmech.2026.119299
PC-3	IC50	0.038 μM	Antiproliferative activity against PC-3 cells assessed as viability reduction incubated 72 hrs by MTT assay. Antiproliferative activity against PC-3 cells assessed as viability reduction incubated 72 hrs by MTT assay.	j.ejmech.2026.119299
HCT-116	IC50	0.053 μM	Antiproliferative activity against HCT-116 cells assessed as viability reduction incubated 72 hrs by MTT assay. Antiproliferative activity against HCT-116 cells assessed as viability reduction incubated 72 hrs by MTT assay.	j.ejmech.2026.119299
4T1	IC50	0.276 μM	Antiproliferative activity against 4T1 cells assessed as viability reduction incubated 72 hrs by MTT assay. Antiproliferative activity against 4T1 cells assessed as viability reduction incubated 72 hrs by MTT assay.	j.ejmech.2026.119299

In Vitro

Anti-cancerApoptosisMitochondrial FunctionOxidative StressOthers

Anti-cancer

CyNPTi-29 (72 h) exhibits low nanomolar antiproliferative activity against tumor cells, with IC₅₀ values of 31 nM in A2780, 38 nM in PC-3, 53 nM in HCT-116, and 276 nM in 4T1 cells; moreover, it shows low cytotoxicity in normal L-02 and HUVEC cells^[1].
CyNPTi-29 (20 μM; 30 min) preferentially accumulates in A2780 and 4T1 tumor cells; it mainly localizes to mitochondria, with PCC values of 0.84 and 0.86, respectively^[1].
OATP1B1/1B3 depletes NAD in A2780 and 4T1 cells, and supplementation with NAM, NMN, or NAD reverses its antiproliferative effect^[1].
CyNPTi-29 (2-4× IC₅₀; 24 h) inhibits the migration of A2780 and 4T1 cells in a concentration-dependent manner^[1].
CyNPTi-29 (2-4× IC₅₀; 10 days) inhibits colony formation in A2780 and 4T1 cells^[1].

Apoptosis

CyNPTi-29 (2× IC₅₀; 3 min NIR) enhances apoptosis in A2780 and 4T1 cells under NIR irradiation, with apoptosis rates increasing to 81.5% and 93.2%, respectively; it also generates ROS^[1].

Mitochondrial Function

CyNPTi-29 exacerbates mitochondrial damage and reduces ATP production in A2780 and 4T1 cells, with stronger effects under NIR irradiation^[1].

Oxidative Stress

CyNPTi-29 (20 nM; 3 min NIR) enhances cytotoxicity against A2780 and 4T1 cells^[1].

Others

CyNPTi-29 retains NAMPT inhibitory activity in cell-free recombinant human NAMPT assays; and exhibits concentration-dependent photothermal heating, reaching 47.2 °C at 20 μM after 3 min of 808 nm irradiation^[1].
CyNPTi-29 (2 μM) combined with NIR irradiation reduces HSP90 expression in A2780 cells^[1].

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

Cell Migration Assay ^[1]

Cell Line:

A2780 and 4T1 cells
Concentration:

2× IC₅₀ and 4× IC₅₀
Incubation Time:

24 h
Result:

Inhibited A2780 and 4T1 cell migration in a concentration-dependent manner, reducing A2780 migration to 55.3% and 7.9% at 2× and 4× IC₅₀.

Cell Proliferation Assay^[1]

Cell Line:

A2780 and 4T1 cells
Concentration:

2× IC₅₀ and 4× IC₅₀
Incubation Time:

10 days
Result:

Suppressed colony formation in A2780 and 4T1 cells, with 4× IC₅₀ almost completely abolishing colony formation.

Apoptosis Analysis^[1]

Cell Line:

A2780 and 4T1 cells
Concentration:

2× IC₅₀
Incubation Time:

3 min (808 nm, 0.2 W/cm2)
Result:

Enhanced apoptosis in A2780 and 4T1 cells under NIR irradiation, with apoptosis rates increasing to 81.5% and 93.2%, respectively.

Cell Viability Assay^[1]

Cell Line:

A2780 and 4T1 cells
Concentration:

A2780: 0, 5, 10, 20, 40 nM
4T1: 0, 50, 100, 200, 400 nM
Incubation Time:

3 min (808 nm, 0.2 W/cm2)
Result:

Enhanced cytotoxicity against A2780 and 4T1 cells.

Parmacokinetics

Species	Dose	Route	T_1/2
Rat^[1]	20 mg/kg	i.v.	0.23 h

In Vivo

Anti-cancer

CyNPTi-29 (10-20 mg/kg; intravenous injection; once every two days; administered seven times within 14 days) produces dose-related tumor growth inhibition and suppresses 4T1 lung metastasis in the 4T1 subcutaneous tumor model^[1].
CyNPTi-29 (10 mg/kg; intravenous injection; single injection; two-week cycle; with or without NIR laser) combined with mPTT achieves 76.3% TGI in the 4T1 subcutaneous tumor model, compared with 53.8% for CyNPTi-29 alone^[1].

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

Animal Model:

BALB/c (female, 1 × 10⁶ 4T1 cells suspension)^[1]
Dosage:

10 mg/kg; 20 mg/kg
Administration:

intravenous; every two days; seven administrations over 14 days
Result:

Produced dose-related tumor growth inhibition in the 4T1 subcutaneous tumor model, with TGI of 56.3% at 10 mg/kg and 78.0% at 20 mg/kg.
Suppressed 4T1 pulmonary metastasis, inhibiting pulmonary nodules by 67.3% at 10 mg/kg and 87.8% at 20 mg/kg.

Related Protocols :

Chemical Information

Molecular Weight 1219.76
Formula C₆₉H₇₈BrClFN₇O₅
SMILES

CC1(C(/C=C/C(CCC/C2=C\C=C3N(C4=C(C\3(C)C)C=CC=C4)CCCCCC(N5CCN(C6=CC=C(C(NCC7=CC=C(NC([C@@H](C8)[C@H]8C9=CC=CN=C9)=O)C=C7F)=O)C=C6)CC5)=O)=C2Cl)=[N+](C%10=CC=CC=C%101)CCCCCC(O)=O)C.[Br-]
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]. Li Z, et al. A hierarchical targeting one-for-all small-molecule enabling multimodal tumor therapy via energy blockade and heat-tolerance suppression. European Journal of Medicinal Chemistry. 2026. Article 119299.

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

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CyNPTi-29

All HSP Isoforms