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[ CAS No. 129497-78-5 ] {[proInfo.proName]}

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Chemical Structure| 129497-78-5
Chemical Structure| 129497-78-5
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Akinduro, Oluwaseun O ; Meade, Paola Suarez ; Schiapparelli, Paula , et al. DOI:

Abstract: Chordomas are locally invasive cancers that are highly resistant to radiotherapy. The Brachyury and Yes Associated Protein (YAP) regulatory axis has been implicated as the primary driver of tumorigenicity in chordoma. Here, we aimed to enhance chordoma radiosensitivity by repurposing the FDA-approved YAP inhibitor, Verteporfin. We used five patient-derived chordoma cell lines and generated two YAP1 knockdown cell lines to validate the YAP-targeting phenotype in chordoma. Verteporfin treatment reduced the expression of DNA damage repair proteins and genes. YAP inhibition with either verteporfin or YAP knockdown resulted in enhanced DNA double-stranded breaks after radiation via inhibition of the DNA damage repair pathway and accumulation of cells in the G2M phase. Verteporfin inhibited chordoma tumor growth alone and in combination with radiation in a xenograft mouse model treated with verteporfin loaded microparticles, resulting in sensitization of chordoma tumors to radiation. YAP inhibition with verteporfin renders chordoma more sensitive to radiation via inhibition of the DNA damage repair cascade and accumulation of cells in G2M when they are most susceptible to radiation damage.

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Akinduro, Oluwaseun O ; Suarez-Meade, Paola ; Roberts, McKinley , et al. DOI: PubMed ID:

Abstract: Objective: The vertebral column is the most common site for skeletal metastasis, often leading to debilitating pain and weakness. Metastatic cancer has unique genetic drivers that potentiate tumorigenicity. There is an unmet need for novel targeted therapy in patients with spinal metastatic disease. Methods: The authors assessed the effect of verteporfin-induced yes-associated protein (YAP) inhibition on spine metastatic cell tumorigenicity and radiation sensitivity in vitro. Animal studies used a subcutaneous xenograft mouse model to assess the use of systemic intraperitoneal verteporfin (IP-VP) and intratumoral verteporfin microparticles (IT-VP) to inhibit the tumorigenicity of lung and breast spinal metastatic tumors from primary patient-derived tissue. Results: Verteporfin led to a dose-dependent decrease in migration, clonogenicity, and cell viability via inhibition of YAP and downstream effectors cyclin D1, CTGF, TOP2A, ANDRD1, MCL-1, FOSL2, KIF14, and KIF23. This was confirmed with knockdown of YAP. Verteporfin has an additive response when combined with radiation, and knockdown of YAP rendered cells more sensitive to radiation. The addition of verteporfin to YAP knockdown cells did not significantly alter migration, clonogenicity, or cell viability. IP-VP and IT-VP led to diminished tumor growth (p < 0.0001), especially when combined with radiation (p < 0.0001). Tissue analysis revealed diminished expression of YAP (p < 0.0001), MCL-1 (p < 0.0001), and Ki-67 (p < 0.0001) in tissue from verteporfin-treated tumors compared with vehicle-treated tumors. Conclusions: This is the first study to demonstrate that verteporfin-mediated inhibition of YAP leads to diminished tumorigenicity in lung and breast spinal metastatic cancer cells. Targeting of YAP with verteporfin offers promising results that could be translated to human clinical trials.

Keywords: YAP ; breast metastasis ; lung cancer ; microparticles ; oncology ; spine metastasis ; verteporfin ; yes-associated protein

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Product Details of [ 129497-78-5 ]

CAS No. :129497-78-5 MDL No. :MFCD28098202
Formula : C41H42N4O8 Boiling Point : -
Linear Structure Formula :- InChI Key :-
M.W : 718.79 Pubchem ID :-
Synonyms :
CL 318952;BPD-MA;DB00460, CL 318952, BPD-MA, BpdMA, Benzoporphyrin D, Benzoporphyrin derivative monoacid ring A, Verteporfin, Visudyne.
Chemical Name :(4R,4aS)-rel-18-Ethenyl-4,4a-dihydro-3,4-bis(methoxycarbonyl)-4a,8,14,19-tetramethyl-24H,26H-Benzo[b]porphine-9,13-dipropanoic acid monomethyl ester

Calculated chemistry of [ 129497-78-5 ]      Expand+

Physicochemical Properties

Num. heavy atoms : 53
Num. arom. heavy atoms : 10
Fraction Csp3 : 0.32
Num. rotatable bonds : 12
Num. H-bond acceptors : 10.0
Num. H-bond donors : 3.0
Molar Refractivity : 210.2
TPSA : 172.5 ?2

Pharmacokinetics

GI absorption : Low
BBB permeant : No
P-gp substrate : Yes
CYP1A2 inhibitor : No
CYP2C19 inhibitor : No
CYP2C9 inhibitor : Yes
CYP2D6 inhibitor : No
CYP3A4 inhibitor : No
Log Kp (skin permeation) : -7.23 cm/s

Lipophilicity

Log Po/w (iLOGP) : 4.75
Log Po/w (XLOGP3) : 4.86
Log Po/w (WLOGP) : 3.5
Log Po/w (MLOGP) : 1.81
Log Po/w (SILICOS-IT) : 8.44
Consensus Log Po/w : 4.67

Druglikeness

Lipinski : 2.0
Ghose : None
Veber : 2.0
Egan : 1.0
Muegge : 2.0
Bioavailability Score : 0.11

Water Solubility

Log S (ESOL) : -6.71
Solubility : 0.000141 mg/ml ; 0.000000197 mol/l
Class : Poorly soluble
Log S (Ali) : -8.22
Solubility : 0.00000436 mg/ml ; 0.0000000061 mol/l
Class : Poorly soluble
Log S (SILICOS-IT) : -8.85
Solubility : 0.00000102 mg/ml ; 0.0000000014 mol/l
Class : Poorly soluble

Medicinal Chemistry

PAINS : 0.0 alert
Brenk : 1.0 alert
Leadlikeness : 3.0
Synthetic accessibility : 8.76

Safety of [ 129497-78-5 ]

Signal Word:Warning Class:N/A
Precautionary Statements:P261-P305+P351+P338 UN#:N/A
Hazard Statements:H302-H315-H319-H335 Packing Group:N/A
GHS Pictogram:
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