PQR626


Catalog No. Size PriceQuantity
M25086-C Contact sales@xcessbio.com for quotation $100Unavailable

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.

Product information

CAS Number: 1927857-98-4

Molecular Weight: 435.47

Formula: C20H27F2N7O2

Chemical Name: 4-(difluoromethyl)-5-{4-[(3R, 5S)-3, 5-dimethylmorpholin-4-yl]-6-[(3R)-3-methylmorpholin-4-yl]-1, 3, 5-triazin-2-yl}pyridin-2-amine

Smiles: C[C@@H]1COCCN1C1=NC(=NC(=N1)C1=CN=C(N)C=C1C(F)F)N1[C@H](C)COC[C@@H]1C

InChiKey: YXQKBQLVKBUCLZ-UPJWGTAASA-N

InChi: InChI=1S/C20H27F2N7O2/c1-11-8-30-5-4-28(11)19-25-18(15-7-24-16(23)6-14(15)17(21)22)26-20(27-19)29-12(2)9-31-10-13(29)3/h6-7,11-13,17H,4-5,8-10H2,1-3H3,(H2,23,24)/t11-,12-,13+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (229.64 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

In Vivo:

PQR626 (10-50 mg/kg; twice a day; for 90 days) reduces the loss of Tsc1-induced mortality as compared to vehicle. 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).

Products are for research use only. Not for human use.

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