Torkinib (PP242)
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MedKoo CAT#: 202324

CAS#: 1092351-67-1

Description: Torkinib, also known as PP242 is a selective mTOR inhibitor with IC50 of 8 nM. PP242 suppresses bladder cancer cell proliferation and migration through deactivating the mammalian target of rapamycin complex 2/AKT1 signaling pathway. PP242 shows strong antitumor activity in a pheochromocytoma PC12 cell tumor model. PP242 suppresses cell proliferation, metastasis, and angiogenesis of gastric cancer through inhibition of the PI3K/AKT/mTOR pathway. PP242 induces apoptosis in AML cells under conditions mimicking the bone marrow microenvironment.


Chemical Structure

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Torkinib (PP242)
CAS# 1092351-67-1

Theoretical Analysis

MedKoo Cat#: 202324
Name: Torkinib (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

Price and Availability

Size Price Availability Quantity
10.0mg USD 150.0 2 Weeks
25.0mg USD 250.0 2 Weeks
50.0mg USD 450.0 2 Weeks
100.0mg USD 650.0 2 Weeks
200.0mg USD 950.0 2 Weeks
500.0mg USD 1650.0 2 Weeks
1.0g USD 2650.0 2 Weeks
2.0g USD 3950.0 2 Weeks
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Synonym: PP242; PP 242; PP-242; Torkinib.

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

InChi Key: MFAQYJIYDMLAIM-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: OC1=CC2=C(NC(C3=NN(C(C)C)C4=NC=NC(N)=C43)=C2)C=C1

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: soluble in DMSO

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 308.33784 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Gordeev SA, Bykova TV, Zubova SG, Bystrova OA, Martynova MG, Pospelov VA, Pospelova TV. mTOR kinase inhibitor pp242 causes mitophagy terminated by apoptotic cell death in E1A-Ras transformed cells. Oncotarget. 2015 Dec 29;6(42):44905-26. doi: 10.18632/oncotarget.6457. PubMed PMID: 26636543; PubMed Central PMCID: PMC4792600.

2: Cheng L, Xia Z, Bian X, Li G, Hu J, Cao Y, Wang Q, Qian X. Combination of cetuximab and PP242 synergistically suppress the progression of wild-type KRAS colorectal carcinoma. Onco Targets Ther. 2015 Nov 2;8:3185-92. doi: 10.2147/OTT.S82453. eCollection 2015. PubMed PMID: 26586952; PubMed Central PMCID: PMC4636092.

3: Zhang Z, Zhang G, Kong C, Gong D. PP242 suppresses bladder cancer cell proliferation and migration through deactivating the mammalian target of rapamycin complex 2/AKT1 signaling pathway. Mol Med Rep. 2016 Jan;13(1):333-8. doi: 10.3892/mmr.2015.4528. Epub 2015 Nov 6. PubMed PMID: 26548560.

4: Benavides-Serrato A, Anderson L, Holmes B, Cloninger C, Artinian N, Bashir T, Gera J. mTORC2 modulates feedback regulation of p38 MAPK activity via DUSP10/MKP5 to confer differential responses to PP242 in glioblastoma. Genes Cancer. 2014 Nov;5(11-12):393-406. PubMed PMID: 25568665; PubMed Central PMCID: PMC4279437.

5: Shi F, Yang X, Gong Y, Shi R, Yang X, Naren D, Wu J. The antileukemia roles of PP242 alone or in combination with daunorubicin in acute leukemia. Anticancer Drugs. 2015 Apr;26(4):410-21. doi: 10.1097/CAD.0000000000000200. PubMed PMID: 25535978.

6: Zhang X, Wang X, Qin L, Xu T, Zhu Z, Zhong S, Zhang M, Shen Z. The dual mTORC1 and mTORC2 inhibitor PP242 shows strong antitumor activity in a pheochromocytoma PC12 cell tumor model. Urology. 2015 Jan;85(1):273.e1-7. doi: 10.1016/j.urology.2014.09.020. Epub 2014 Nov 6. PubMed PMID: 25440763.

7: Qin Y, Zhao X, Fang Y. PP242 synergizes with suberoylanilide hydroxamic acid to inhibit growth of ovarian cancer cells. Int J Gynecol Cancer. 2014 Oct;24(8):1373-80. doi: 10.1097/IGC.0000000000000238. PubMed PMID: 25188886.

8: Xing X, Zhang L, Wen X, Wang X, Cheng X, Du H, Hu Y, Li L, Dong B, Li Z, Ji J. PP242 suppresses cell proliferation, metastasis, and angiogenesis of gastric cancer through inhibition of the PI3K/AKT/mTOR pathway. Anticancer Drugs. 2014 Nov;25(10):1129-40. doi: 10.1097/CAD.0000000000000148. PubMed PMID: 25035961; PubMed Central PMCID: PMC4222793.

9: Ono A, Oike R, Okuhashi Y, Takahashi Y, Itoh M, Nara N, Tohda S. Comparative effects of PP242 and rapamycin on mTOR signalling and NOTCH signalling in leukemia cells. Anticancer Res. 2013 Mar;33(3):809-13. PubMed PMID: 23482748.

10: Zeng Z, Shi YX, Tsao T, Qiu Y, Kornblau SM, Baggerly KA, Liu W, Jessen K, Liu Y, Kantarjian H, Rommel C, Fruman DA, Andreeff M, Konopleva M. Targeting of mTORC1/2 by the mTOR kinase inhibitor PP242 induces apoptosis in AML cells under conditions mimicking the bone marrow microenvironment. Blood. 2012 Sep 27;120(13):2679-89. Epub 2012 Jul 23. PubMed PMID: 22826565; PubMed Central PMCID: PMC3460689.

11: Hoang B, Benavides A, Shi Y, Yang Y, Frost P, Gera J, Lichtenstein A. The PP242 mammalian target of rapamycin (mTOR) inhibitor activates extracellular signal-regulated kinase (ERK) in multiple myeloma cells via a target of rapamycin complex 1 (TORC1)/eukaryotic translation initiation factor 4E (eIF-4E)/RAF pathway and activation is a mechanism of resistance. J Biol Chem. 2012 Jun 22;287(26):21796-805. doi: 10.1074/jbc.M111.304626. Epub 2012 May 3. PubMed PMID: 22556409; PubMed Central PMCID: PMC3381142.



Additional Information

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.
 
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