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MedKoo product information:
PP242
PP242 is a novel potent and selective mTOR inhibitor with an IC50 of
8 nM. PP242 also shows residual (micromolar) activity against panel
of tyrosine kinases. But PP242 was much less active against other
PI3K family members with IC50 of 2, 2.2, 0.1, 1.3 and 0.41 μM for
p110α, p110β, p110δ, p110γ and DNA-PK, respectively.
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MedKoo Code#:
202324
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Name:
Pp242
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CAS#:
1092351-67-1
Synonym:
Pp242
IUPAC/Chemical name:
2-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol
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Chemical structure
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Theoretical analysis
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MedKoo Code#: 202324
Name: PP242
CAS#: 1092351-67-1
Chemical Formula: C16H16N6O
Exact Mass: 308.13856
Molecular Weight: 308.33784
Elemental Analysis: C, 62.32; H, 5.23; N,
27.26; O, 5.19
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Availability and price:
This agent (99%) is in stock.
10 mg /
$190.00
50 mg / $450.00
100 mg / $750.00
200 mg / $1,150.00
To inquire quotation and lead time or to ask questions, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
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Information about this agent
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Pp242 is a novel potent and selective mTOR inhibitor.
Inhibits mTOR kinase with IC50 = 8 nM nad PI3 kinase (PI3K), with p110α
IC50 = 2000 nM, p110b IC50 = 2200 nM, p110d IC50 = 100 nM, p110g IC50 =
1300 nM and DNA-PK IC50 = 410 nM. It also shows residual (micromolar)
activity against panel of tyrosine kinases.
Current developer:
1: Frégeau MO, Régimbald-Dumas Y, Guillemette
G. Positive regulation of inositol 1,4,5-trisphosphate-induced Ca(2+)
release by mammalian target of rapamycin (mTOR) in RINm5F cells. J Cell
Biochem. 2010 Dec 29. [Epub ahead of print] PubMed PMID: 21191991.
2: Song X, Kusakari Y, Xiao CY, Kinsella SD, Rosenberg MA,
Scherrer-Crosbie M, Hara K, Rosenzweig A, Matsui T. mTOR attenuates the
inflammatory response in cardiomyocytes and prevents cardiac dysfunction
in pathological hypertrophy. Am J Physiol Cell Physiol. 2010
Dec;299(6):C1256-66. Epub 2010 Sep 22. PubMed PMID: 20861467.
3: Mansley MK, Wilson SM. Dysregulation of epithelial Na+ absorption
induced by inhibition of the kinases TORC1 and TORC2. Br J Pharmacol.
2010 Dec;161(8):1778-92. doi: 10.1111/j.1476-5381.2010.01003.x. PubMed
PMID: 20735411.
4: Hoang B, Frost P, Shi Y, Belanger E, Benavides A, Pezeshkpour G,
Cappia S, Guglielmelli T, Gera J, Lichtenstein A. Targeting TORC2 in
multiple myeloma with a new mTOR kinase inhibitor. Blood. 2010 Nov
25;116(22):4560-8. Epub 2010 Aug 4. PubMed PMID: 20686120; PubMed
Central PMCID: PMC2996116.
5: Cai H, Das S, Kamimura Y, Long Y, Parent CA, Devreotes PN. Ras-mediated
activation of the TORC2-PKB pathway is critical for chemotaxis. J Cell
Biol. 2010 Jul 26;190(2):233-45. PubMed PMID: 20660630; PubMed Central
PMCID: PMC2930282.
6: Hsieh AC, Costa M, Zollo O, Davis C, Feldman ME, Testa JR, Meyuhas O,
Shokat KM, Ruggero D. Genetic dissection of the oncogenic mTOR pathway
reveals druggable addiction to translational control via 4EBP-eIF4E.
Cancer Cell. 2010 Mar 16;17(3):249-61. PubMed PMID: 20227039; PubMed
Central PMCID: PMC2901095.
7: Janes MR, Limon JJ, So L, Chen J, Lim RJ, Chavez MA, Vu C, Lilly MB,
Mallya S, Ong ST, Konopleva M, Martin MB, Ren P, Liu Y, Rommel C, Fruman
DA. Effective and selective targeting of leukemia cells using a TORC1/2
kinase inhibitor. Nat Med. 2010 Feb;16(2):205-13. Epub 2010 Jan 13.
PubMed PMID: 20072130.
8: Sturgill TW, Hall MN. Activating mutations in TOR are in similar
structures as oncogenic mutations in PI3KCalpha. ACS Chem Biol. 2009 Dec
18;4(12):999-1015. PubMed PMID: 19902965; PubMed Central PMCID:
PMC2796128.
9: Feldman ME, Apsel B, Uotila A, Loewith R, Knight ZA, Ruggero D,
Shokat KM. Active-site inhibitors of mTOR target rapamycin-resistant
outputs of mTORC1 and mTORC2. PLoS Biol. 2009 Feb 10;7(2):e38. PubMed
PMID: 19209957; PubMed Central PMCID: PMC2637922.
10: Sammons CC, Sweet C. Isolation and preliminary characterization of
temperature-sensitive mutants of mouse cytomegalovirus of differing
virulence for 1-week-old mice. J Gen Virol. 1989 Sep;70 ( Pt 9):2373-81.
PubMed PMID: 2550573.
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