PP242 (Torkinib)

Catalog No. A10746

PP242 (Torkinib)在mTORC1和mTORC2中都是有效的选择性mTOR抑制剂。

Product Citations

Hiroshi Fukamachi, .et al. A subset of diffuse-type gastric cancer is susceptible to mTOR inhibitors and checkpoint inhibitors, J Exp Clin Cancer Res, 2019, 38:127
Fuse MJ, .et al. Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers, Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539

Technical details

Catalog Num	A10746
M. Wt	308.3
Formula	C16H16N6O
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1092351-67-1
Synonyms	PP-242
SMILES	CC(C)N1C2=C(/C(=C\3/C=C4C=C(C=CC4=N3)O)/N1)C(=NC=N2)N

Biological Activity

PP242 (Torkinib)在mTORC1和mTORC2中都是有效的选择性mTOR抑制剂。

Targets

Target	Value
mTOR	IC50: 8nM
p110δ	IC50: 0.10μM
DNA-PK	IC50: 0.41μM
PDGFR	IC50: 0.41μM
Hck	IC50: 1.2μM
p110γ	IC50: 1.3μM
Src	IC50: 1.4μM
VEGFR2	IC50: 1.5μM
p110α	IC50: 2.0μM
p110β	IC50: 2.2μM
EphB4	IC50: 3.4μM
Abl	IC50: 3.6μM
EGFR	IC50: 4.4μM
Src(T338I)	IC50: 5.1μM

Solubility *

In vitro (25°C)	DMSO	57 mg/mL (184.86 mM)
	Water	Insoluble
	Ethanol	17 mg/mL (55.13 mM)
In vivo	2% DMSO+30% PEG 300+5% Tween 80+ddH2O	4 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	32.44 mL	162.18 mL	324.36 mL
0.5 mM	6.49 mL	32.44 mL	64.87 mL
1 mM	3.24 mL	16.22 mL	32.44 mL
5 mM	0.65 mL	3.24 mL	6.49 mL

*The above data is based on the productmolecular weight 308.3 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.