PP242 --- mTORC1/mTORC2 inhibitor


Catalog No. size PriceQuantity
M60094-5S 5 mg solid $69
M60094-50S 50mg solid $370

Description

PP242 is a highly potent, selective and ATP-competitive mTORC1/mTORC2 inhibitor (IC50 = 8 nM). It has > 10 folds selectivity over the other PI-3K family kinases (IC50 0.102 µM, 0.408 µM, 1.27 µM, 1.96 µM and 2.2 μM for p110γ, DNA-PK, p110δ, p110α and p110β, respectively). Except some weak inhibitory activity against PKCα, JAK2, PKCβI, PKCβII and RET (0.05-0.22 µM), PP242 exhibits excellent selectivity over 215 other protein kinases. PP242 differentially inhibits insulin-stimulated phosphorylations of cellular proteins both in vitro and in vivo in a manner distinctly different from that seen in mTORC2-functional knockout SIN1-/- cells or in cultures treated with Rapamycin, which targets only mTORC1, but not mTORC2. Blockage of 4EBP1 T36/T45/S65 phosphorylation by PP242 upon insulin stimulation in primary MEFs correlates well with an enhanced 4EBP1 association with the cap-binding protein eIF4E, resulting in a selective inhibition of cap-dependent, but not cap-independent, protein translation.

Product information

CAS Number: 1092351-67-1

Molecular Weight: 308.34

Formula: C16H16N6O

Synonym:

Torkinib

Chemical Name: 2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol

Smiles: CC(C)N1N=C(C2=C(N)N=CN=C12)C1=CC2=CC(O)=CC=C2N1

InChiKey: MFAQYJIYDMLAIM-UHFFFAOYSA-N

InChi: InChI=1S/C16H16N6O/c1-8(2)22-16-13(15(17)18-7-19-16)14(21-22)12-6-9-5-10(23)3-4-11(9)20-12/h3-8,20,23H,1-2H3,(H2,17,18,19)

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO up to 100 mM

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:

PP242 was used at 2.5 µM concentration in vitro and in cellular assays.

In Vivo:

PP242 was orally dosed to mice at 20-60 mg/kg once per day to inhibit tumor growth, or in combination with Dasatinib, Bortezomib or Imatinib for synergistic activity.

References:

  1. Feldman ME, et al. Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. (2009) PLoS Biol. 7(2):e38.
  2. Janes MR, et al. Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor.(2010) Nat Med. 16(2):205-13.
  3. Hoang B, et al. Targeting TORC2 in multiple myeloma with a new mTOR kinase inhibitor. (2010) Blood. 116(22):4560-8.
  4. Liu Q, et al. Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics. (2012) J Biol Chem. 287(13):9742-52.

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


Documents

Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed