1. PI3K/Akt/mTOR
  2. mTOR
  3. PQR626

PQR626, a rapamycin derivative, is a potent, selective, orally active, and brain-penetrant mTOR inhibitor, with an IC50 and Ki of 5 nM and 3.6 nM, respectively. PQR626 can be can be used for the research of neurological disorders.

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

PQR626 Chemical Structure

PQR626 Chemical Structure

CAS No. : 1927857-98-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 451 In-stock
Solution
10 mM * 1 mL in DMSO USD 451 In-stock
Solid
5 mg USD 410 In-stock
10 mg USD 710 In-stock
25 mg USD 1100 In-stock
50 mg USD 2000 In-stock
100 mg USD 3100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

PQR626, a rapamycin derivative, is a potent, selective, orally active, and brain-penetrant mTOR inhibitor, with an IC50 and Ki of 5 nM and 3.6 nM, respectively. PQR626 can be can be used for the research of neurological disorders[1][2].

IC50 & Target

IC50: 5 nM (mTOR)[1]

In Vitro

PQR626 (0.04-5 μΜ; 1 hour) has IC50s of 197 nM and 87 nM for pPKB S473 and pS6 S235/S236, respectively, in-cell western blot. S6 kinase (S6K), S6 ribosomal protein (S6rP) and 4E-binding protein (4E-BP) are prominent downstream effectors of mTOR[1].

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

Western Blot Analysis[1]

Cell Line: A2058 cells
Concentration: 0.04 μΜ, 0.08 μΜ, 0.155 μΜ, 0.3125 μΜ, 0.625 μΜ, 1.25 μΜ, 5 μΜ
Incubation Time: 1 hour
Result: Inhibited mTOR in cell.
In Vivo

PQR626 (10-50 mg/kg; twice a day; for 90 days) reduces the loss of Tsc1-induced mortality as compared to vehicle[2].
PQR626 exhibits terminal elimination half-life (mice 3.0 h) due to high plasma clearance (1096 ng/mL) following oral dosing (10 mg/kg; p.o.; daily; for 4 days)[2].

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

Animal Model: BALB/c nude female mice, Tsc1GFAP CKO mice model[2]
Dosage: 10 mg/kg, 25 mg/kg, 50 mg/kg
Administration: Oral administration, twice a day, for 90 days
Result: Significantly reduced the loss of Tsc1-induced mortality.
Animal Model: Female C57BL/6J Mice[1]
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration, daily, for 4 days
Result: Cmax (1096 ng/mL), T1/2 (3.0 h).
Molecular Weight

435.47

Formula

C20H27F2N7O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

NC1=NC=C(C2=NC(N3[C@H](C)COC[C@@H]3C)=NC(N4[C@H](C)COCC4)=N2)C(C(F)F)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (229.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2964 mL 11.4818 mL 22.9637 mL
5 mM 0.4593 mL 2.2964 mL 4.5927 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2964 mL 11.4818 mL 22.9637 mL 57.4092 mL
5 mM 0.4593 mL 2.2964 mL 4.5927 mL 11.4818 mL
10 mM 0.2296 mL 1.1482 mL 2.2964 mL 5.7409 mL
15 mM 0.1531 mL 0.7655 mL 1.5309 mL 3.8273 mL
20 mM 0.1148 mL 0.5741 mL 1.1482 mL 2.8705 mL
25 mM 0.0919 mL 0.4593 mL 0.9185 mL 2.2964 mL
30 mM 0.0765 mL 0.3827 mL 0.7655 mL 1.9136 mL
40 mM 0.0574 mL 0.2870 mL 0.5741 mL 1.4352 mL
50 mM 0.0459 mL 0.2296 mL 0.4593 mL 1.1482 mL
60 mM 0.0383 mL 0.1914 mL 0.3827 mL 0.9568 mL
80 mM 0.0287 mL 0.1435 mL 0.2870 mL 0.7176 mL
100 mM 0.0230 mL 0.1148 mL 0.2296 mL 0.5741 mL
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PQR626 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PQR626
Cat. No.:
HY-136660
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