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MedKoo Cat#: 202324 | Name: Torkinib
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

Torkinib
Torkinib
CAS#1092351-67-1

Theoretical Analysis

MedKoo Cat#: 202324

Name: Torkinib

CAS#: 1092351-67-1

Chemical Formula: C16H16N6O

Exact Mass: 308.1386

Molecular Weight: 308.34

Elemental Analysis: C, 62.32; H, 5.23; N, 27.26; O, 5.19

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,650.00 2 Weeks
1g USD 3,850.00 2 Weeks
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Related CAS #
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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
More Info
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:       

Preparing Stock Solutions

The following data is based on the product molecular weight 308.34 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
1: Machova Urdzikova L, Cimermanova V, Karova K, Dominguez J, Stepankova K, Petrovicova M, Havelikova K, D Gandhi C, Jhanwar-Uniyal M, Jendelova P. The Role of Green Tea Catechin Epigallocatechin Gallate (EGCG) and Mammalian Target of Rapamycin (mTOR) Inhibitor PP242 (Torkinib) in the Treatment of Spinal Cord Injury. Antioxidants (Basel). 2023 Feb 3;12(2):363. doi: 10.3390/antiox12020363. PMID: 36829922; PMCID: PMC9952296. 2: Koo J, Yue P, Deng X, Khuri FR, Sun SY. mTOR Complex 2 Stabilizes Mcl-1 Protein by Suppressing Its Glycogen Synthase Kinase 3-Dependent and SCF- FBXW7-Mediated Degradation. Mol Cell Biol. 2015 Jul;35(13):2344-55. doi: 10.1128/MCB.01525-14. Epub 2015 Apr 27. PMID: 25918246; PMCID: PMC4456440. 3: Zhou K, Chen X, Zhang L, Yang Z, Zhu H, Guo D, Su R, Chen H, Li H, Song P, Xu X, Wang H, Zheng S, Xie H. Targeting peripheral immune organs with self- assembling prodrug nanoparticles ameliorates allogeneic heart transplant rejection. Am J Transplant. 2021 Dec;21(12):3871-3882. doi: 10.1111/ajt.16748. Epub 2021 Jul 19. PMID: 34212503. 4: Parate S, Kumar V, Lee G, Rampogu S, Hong JC, Lee KW. Marine-Derived Natural Products as ATP-Competitive mTOR Kinase Inhibitors for Cancer Therapeutics. Pharmaceuticals (Basel). 2021 Mar 21;14(3):282. doi: 10.3390/ph14030282. PMID: 33801030; PMCID: PMC8003863. 5: 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. doi: 10.1371/journal.pbio.1000038. PMID: 19209957; PMCID: PMC2637922. 6: Pham AM, Kwun HJ. Casein kinase 1α mediates phosphorylation of the Merkel cell polyomavirus large T antigen for β-TrCP destruction complex interaction and subsequent degradation. mBio. 2024 Aug 14;15(8):e0111724. doi: 10.1128/mbio.01117-24. Epub 2024 Jun 28. PMID: 38940554; PMCID: PMC11323502. 7: Li P, He J, Yang Z, Ge S, Zhang H, Zhong Q, Fan X. ZNNT1 long noncoding RNA induces autophagy to inhibit tumorigenesis of uveal melanoma by regulating key autophagy gene expression. Autophagy. 2020 Jul;16(7):1186-1199. doi: 10.1080/15548627.2019.1659614. Epub 2019 Sep 3. PMID: 31462126; PMCID: PMC7469589. 8: Ciołczyk-Wierzbicka D, Krawczyk A, Zarzycka M, Zemanek G, Wierzbicki K. Three generations of mTOR kinase inhibitors in the activation of the apoptosis process in melanoma cells. J Cell Commun Signal. 2023 Sep;17(3):975-989. doi: 10.1007/s12079-023-00748-9. Epub 2023 Apr 25. Erratum in: J Cell Commun Signal. 2023 Sep;17(3):991. doi: 10.1007/s12079-023-00764-9. PMID: 37097377; PMCID: PMC10409930. 9: Suwannalert P, Panpinyaporn P, Wantanachaisaeng P, Teeppaibul T, Khumsri W, Koomsang T, Payuhakrit W, Naktubtim C. A Potential Combination of Targeting HSP90 and mTOR in Breast Cancer Cell Growth, Migration, and Invasion Through Inhibiting AKT Phosphorylation and F-actin Organization. Anticancer Res. 2024 Jun;44(6):2555-2565. doi: 10.21873/anticanres.17061. PMID: 38821604.

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