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Chemical Structure| 934526-89-3 Chemical Structure| 934526-89-3

Structure of Pilaralisib
CAS No.: 934526-89-3

Chemical Structure| 934526-89-3

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XL147 is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases with IC50 values of 39 nM/383 nM/36 nM/23 nM for PI3Kα/β/δ/γ, respectively and less potent to PI3Kβ.

Synonyms: XL147

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Product Details of Pilaralisib

CAS No. :934526-89-3
Formula : C25H25ClN6O4S
M.W : 541.02
SMILES Code : ClC1=C(C=C(C=C1)OC)NC2=NC3=CC=CC=C3N=C2NS(C4=CC(NC(C(C)(C)N)=O)=CC=C4)(=O)=O
Synonyms :
XL147
MDL No. :MFCD26142605
InChI Key :QINPEPAQOBZPOF-UHFFFAOYSA-N
Pubchem ID :56599306

Safety of Pilaralisib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Pilaralisib

PI3K-AKT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HCC1954 10 µM 24 hours XL147 + trastuzumab inhibited proliferation and growth of HCC1954 cells PMC3563941
MDA453 cells 6 μM 48 h Measure HER3 mRNA levels, found significant increase after XL147 treatment PMC3286932
SKBR3 cells 6 μM 48 h Measure HER3 mRNA levels, found significant increase after XL147 treatment PMC3286932
HR6 6 µM 5 days XL147 + trastuzumab inhibited proliferation and growth of HR6 cells PMC3563941
HR5 6 µM 5 days XL147 + trastuzumab inhibited proliferation and growth of HR5 cells PMC3563941
CFBE41o− cells 3 µM 24 hours To evaluate the rescue effect of XL147 on ΔF508-CFTR function, results showed that XL147 partially restored ΔF508-CFTR function. PMC8846631
PyVmT cells 25 nM 24, 48, 72 hours Evaluate the effect of XL147 on metabolic heterogeneity in PyVmT cells, results showed XL147 significantly reduced OMI index and metabolic heterogeneity PMC6514366
HR6 cells 10 nM 24, 48, 72 hours Evaluate the drug response of XL147 on HR6 cells, showing a significant decrease in OMI index at 24 and 48 hours, but no significant change at 72 hours. PMC5480588
BT474 cells 10 nM 24, 48, 72 hours Evaluate the drug response of XL147 on BT474 cells, showing a significant decrease in OMI index at all time points. PMC5480588
MCF10A cells 1 μM 3 hours To evaluate the inhibitory effect of Pilaralisib on HER2T798M mutant cells. Results showed that Pilaralisib could inhibit the growth and signaling of HER2T798M mutant cells. PMC3809918
BT474 cells 1 μM 3 hours To evaluate the inhibitory effect of Pilaralisib on HER2T798M mutant cells. Results showed that Pilaralisib could inhibit the growth and signaling of HER2T798M mutant cells. PMC3809918
BT474 cells 6 μM 6 h Measure HER3 mRNA levels, found significant increase after XL147 treatment PMC3286932
HCC1569 6 µM 24 hours XL147 + trastuzumab inhibited proliferation and growth of HCC1569 cells PMC3563941
SUM190 6 µM 24 hours XL147 + trastuzumab inhibited proliferation and growth of SUM190 cells PMC3563941

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Athymic female mice HR6 xenografts Orally 100 mg/kg XL147 daily, trastuzumab twice weekly, for 28 days XL147 + trastuzumab significantly inhibited the growth of HR6 xenografts PMC3563941
Nude mice BT474T798M xenograft model Oral gavage 100 mg/kg Once daily for 4-5 weeks To evaluate the inhibitory effect of Pilaralisib on HER2T798M mutant tumors in vivo. Results showed that Pilaralisib could significantly inhibit tumor growth. PMC3809918
Mice Gastrointestinal stromal tumor model Oral gavage 100 mg/kg Once daily for 7 days To evaluate the therapeutic effect of Pilaralisib on gastrointestinal stromal tumors, results showed inhibition of PI3K signaling pathway and reduced tumor cell proliferation. PMC5635919
NIH Swiss mice Lung squamous cell carcinoma model Oral gavage 100 mg/kg 5 days a week for 4 weeks To study the therapeutic effect of XL-147 on lung squamous cell carcinoma and the potential of exosomal miRNAs as pharmacodynamic biomarkers PMC6520832
FVB mice PyVmT breast cancer model Oral gavage 50 mg/kg Once daily for 14 days Evaluate the effect of XL147 on tumor growth and metabolic heterogeneity in PyVmT tumors, results showed XL147 combined with paclitaxel significantly reduced tumor growth and metabolic heterogeneity PMC6514366

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.18mL

9.24mL

1.85mL

0.92mL

18.48mL

3.70mL

1.85mL

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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