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  3. PQR530

PQR530 

Cat. No.: HY-107365
Handling Instructions

PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity.

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

PQR530 Chemical Structure

PQR530 Chemical Structure

CAS No. : 1927857-61-1

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 220 In-stock
Estimated Time of Arrival: December 31
5 mg USD 200 In-stock
Estimated Time of Arrival: December 31
10 mg USD 300 In-stock
Estimated Time of Arrival: December 31
25 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 850 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity[1][2].

IC50 & Target[2]

mTOR

0.33 nM (Kd)

PI3Kα

0.84 nM (Kd)

PI3Kβ

6.1 nM (Kd)

PI3Kγ

10 nM (Kd)

PI3Kδ

11 nM (Kd)

PI3KC2β

100 nM (Kd)

In Vitro

PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity. PQR-530 inhibits all PI3K isoforms and mTOR complexes C1/2 potently and selectively. PQR-530 inhibits protein kinase B (PKB, pSer473) and ribosomal protein S6 (pS6, pSer235/236) phosphorylation with IC50 values of 0.07 µM in A2058 melanoma cells. PQR-530 shows inhibitory activity against the growth of 44 cancer cell lines with mean GI50 of 426 nM[1].

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

Molecular Weight

407.42

Formula

C₁₈H₂₃F₂N₇O₂

CAS No.

1927857-61-1

SMILES

FC(C1=CC(N)=NC=C1C2=NC(N3CCOCC3)=NC(N4[[email protected]](COCC4)C)=N2)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

PQR530PQR 530PQR-530PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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PQR530
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HY-107365
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