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MedKoo Cat#: 564620 | Name: OSU-T315 (1,5-regioisomer)
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Description:

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

OSU-T315 (1,5-regioisomer) is a potent and specific integrin-linked kinase (ILK) inhibitor which inhibits PDK2 function in the AKT pathway activation, showing a specific mechanism of abrogating the AKT pathway and inhibition of BCR activity in the leukemic cell. OSU-T315 also acts as a selective inhibitor of biofilm formation.

Chemical Structure

OSU-T315 (1,5-regioisomer)
OSU-T315 (1,5-regioisomer)
CAS#1333146-24-9

Theoretical Analysis

MedKoo Cat#: 564620

Name: OSU-T315 (1,5-regioisomer)

CAS#: 1333146-24-9

Chemical Formula: C30H30F3N5O

Exact Mass: 533.2402

Molecular Weight: 533.60

Elemental Analysis: C, 67.53; H, 5.67; F, 10.68; N, 13.13; O, 3.00

Price and Availability

Size Price Availability Quantity
5mg USD 400.00 2 Weeks
10mg USD 750.00 2 Weeks
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Related CAS #
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Synonym
ILK inhibitor 22(1,5); T315(1,5); OSU-T315 (1,5-regioisomer); OSUT315; OSU T315; OSU-T315; CPD 22; CPD22; CPD-22
IUPAC/Chemical Name
N-Methyl-3-[1-(4-piperazin-1-yl-phenyl)-5-(4'-trifluoromethyl-biphenyl-4-yl)-1H-pyrazol-3-yl]-propionamide
InChi Key
GHBUPSVATJKTRR-UHFFFAOYSA-N
InChi Code
InChI=1S/C30H30F3N5O/c1-34-29(39)15-10-25-20-28(38(36-25)27-13-11-26(12-14-27)37-18-16-35-17-19-37)23-4-2-21(3-5-23)22-6-8-24(9-7-22)30(31,32)33/h2-9,11-14,20,35H,10,15-19H2,1H3,(H,34,39)
SMILES Code
O=C(NC)CCC1=NN(C2=CC=C(N3CCNCC3)C=C2)C(C4=CC=C(C5=CC=C(C(F)(F)F)C=C5)C=C4)=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
>3 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
2934.99.03.00
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor.
In vitro activity:
OSU-T315 decreased cell viability at IC50 < 2μM in VS (HEI193) and meningioma (Ben-Men-1) cell lines, in primary cells at < 3.5μM, while in normal primary Schwann cells at 7.1μM. OSU-T315 inhibits AKT signaling by decreasing phosphorylation at AKT-Ser473, AKT-Thr308, ILK-Ser246 and ILK-Thr173. In addition, OSU-T315 affected the phosphorylation or expression levels of AKT downstream proliferation effectors as well as autophagy markers. Reference: Austin J Med Oncol. 2016;3(1):1025. https://pubmed.ncbi.nlm.nih.gov/27642646/
In vivo activity:
Mice that developed leukemia in the bloodstream (≥10% CD5+/CD19+ cells) were treated orally with vehicle or OSU-T315 (50 mg/kg daily). Mice that received OSU-T315 show significantly reduced white blood cell (WBC) counts after 4 weeks of treatment (P = .036; n = 6 per group; Figure 6A). This improvement also correlated with prolonged overall survival in the OSU-T315-treated group (P = .037; n = 6 per group; Figure 6B). Reference: Blood. 2015 Jan 8;125(2):284-95. https://pubmed.ncbi.nlm.nih.gov/25293770/
Solvent mg/mL mM
Solubility
DMSO 50.0 93.70
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 533.60 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
Formulation protocol:
1. Guo Y, Feng L. N6-methyladenosine-mediated upregulation of LINC00520 accelerates breast cancer progression via regulating miR-577/POSTN axis and downstream ILK/AKT/mTOR signaling pathway. Arch Biochem Biophys. 2022 Oct 30;729:109381. doi: 10.1016/j.abb.2022.109381. Epub 2022 Aug 23. PMID: 36027936. 2. Mercado-Pimentel ME, Igarashi S, Dunn AM, Behbahani M, Miller C, Read CM, Jacob A. The Novel Small Molecule Inhibitor, OSU-T315, Suppresses Vestibular Schwannoma and Meningioma Growth by Inhibiting PDK2 Function in the AKT Pathway Activation. Austin J Med Oncol. 2016;3(1):1025. Epub 2016 Apr 21. PMID: 27642646; PMCID: PMC5024787. 3. Van Belle K, Herman J, Waer M, Sprangers B, Louat T. OSU-T315 as an Interesting Lead Molecule for Novel B Cell-Specific Therapeutics. J Immunol Res. 2018 Sep 12;2018:2505818. doi: 10.1155/2018/2505818. PMID: 30276218; PMCID: PMC6157143. 4. Liu TM, Ling Y, Woyach JA, Beckwith K, Yeh YY, Hertlein E, Zhang X, Lehman A, Awan F, Jones JA, Andritsos LA, Maddocks K, MacMurray J, Salunke SB, Chen CS, Phelps MA, Byrd JC, Johnson AJ. OSU-T315: a novel targeted therapeutic that antagonizes AKT membrane localization and activation of chronic lymphocytic leukemia cells. Blood. 2015 Jan 8;125(2):284-95. doi: 10.1182/blood-2014-06-583518. Epub 2014 Oct 7. PMID: 25293770; PMCID: PMC4287637.
In vitro protocol:
1. Guo Y, Feng L. N6-methyladenosine-mediated upregulation of LINC00520 accelerates breast cancer progression via regulating miR-577/POSTN axis and downstream ILK/AKT/mTOR signaling pathway. Arch Biochem Biophys. 2022 Oct 30;729:109381. doi: 10.1016/j.abb.2022.109381. Epub 2022 Aug 23. PMID: 36027936. 2. Mercado-Pimentel ME, Igarashi S, Dunn AM, Behbahani M, Miller C, Read CM, Jacob A. The Novel Small Molecule Inhibitor, OSU-T315, Suppresses Vestibular Schwannoma and Meningioma Growth by Inhibiting PDK2 Function in the AKT Pathway Activation. Austin J Med Oncol. 2016;3(1):1025. Epub 2016 Apr 21. PMID: 27642646; PMCID: PMC5024787.
In vivo protocol:
1. Van Belle K, Herman J, Waer M, Sprangers B, Louat T. OSU-T315 as an Interesting Lead Molecule for Novel B Cell-Specific Therapeutics. J Immunol Res. 2018 Sep 12;2018:2505818. doi: 10.1155/2018/2505818. PMID: 30276218; PMCID: PMC6157143. 2. Liu TM, Ling Y, Woyach JA, Beckwith K, Yeh YY, Hertlein E, Zhang X, Lehman A, Awan F, Jones JA, Andritsos LA, Maddocks K, MacMurray J, Salunke SB, Chen CS, Phelps MA, Byrd JC, Johnson AJ. OSU-T315: a novel targeted therapeutic that antagonizes AKT membrane localization and activation of chronic lymphocytic leukemia cells. Blood. 2015 Jan 8;125(2):284-95. doi: 10.1182/blood-2014-06-583518. Epub 2014 Oct 7. PMID: 25293770; PMCID: PMC4287637.
1: Huang Z, Huang L, Ding J, Huang Y, Huang X, Li T. ILK inhibition reduces osteophyte formation through suppression of osteogenesis in BMSCs via Akt/GSK-3β/β-catenin pathway. Mol Biol Rep. 2024 Mar 14;51(1):421. doi: 10.1007/s11033-024-09336-5. PMID: 38483756. 2: Guo Y, Feng L. N6-methyladenosine-mediated upregulation of LINC00520 accelerates breast cancer progression via regulating miR-577/POSTN axis and downstream ILK/AKT/mTOR signaling pathway. Arch Biochem Biophys. 2022 Oct 30;729:109381. doi: 10.1016/j.abb.2022.109381. Epub 2022 Aug 23. PMID: 36027936. 3: Li Z, Ren D, Chen C, Sun L, Fang K. OSU-T315 and doxorubicin synergistically induce apoptosis via mitochondrial pathway in bladder cancer cells. Cell Biol Int. 2022 Oct;46(10):1672-1681. doi: 10.1002/cbin.11855. Epub 2022 Jul 13. PMID: 35830716. 4: Chen H, Cheng M, Gao P, Zhang X, Li G, Wang L, Qin L, Li H. GDC-0941 activates integrin linked kinase (ILK) expression to cause resistance to GDC-0941 in breast cancer by the tumor necrosis factor (TNF)-α signaling pathway. Bioengineered. 2022 Apr;13(4):10944-10955. doi: 10.1080/21655979.2022.2066758. PMID: 35477364; PMCID: PMC9208486. 5: Tsai MS, Chen SH, Chang CP, Hsiao YL, Wang LC. Integrin-Linked Kinase Reduces H3K9 Trimethylation to Enhance Herpes Simplex Virus 1 Replication. Front Cell Infect Microbiol. 2022 Mar 8;12:814307. doi: 10.3389/fcimb.2022.814307. PMID: 35350437; PMCID: PMC8957879. 6: Li B, Wang X, Wang R, Rutz B, Ciotkowska A, Gratzke C, Herlemann A, Spek A, Tamalunas A, Waidelich R, Stief CG, Hennenberg M. Inhibition of neurogenic and thromboxane A2 -induced human prostate smooth muscle contraction by the integrin α2β1 inhibitor BTT-3033 and the integrin-linked kinase inhibitor Cpd22. Prostate. 2020 Aug;80(11):831-849. doi: 10.1002/pros.23998. Epub 2020 May 25. PMID: 32449814. 7: Van Belle K, Herman J, Waer M, Sprangers B, Louat T. OSU-T315 as an Interesting Lead Molecule for Novel B Cell-Specific Therapeutics. J Immunol Res. 2018 Sep 12;2018:2505818. doi: 10.1155/2018/2505818. PMID: 30276218; PMCID: PMC6157143. 8: Mercado-Pimentel ME, Igarashi S, Dunn AM, Behbahani M, Miller C, Read CM, Jacob A. The Novel Small Molecule Inhibitor, OSU-T315, Suppresses Vestibular Schwannoma and Meningioma Growth by Inhibiting PDK2 Function in the AKT Pathway Activation. Austin J Med Oncol. 2016;3(1):1025. Epub 2016 Apr 21. PMID: 27642646; PMCID: PMC5024787. 9: Robak T, Smolewski P. Novel target to kill CLL. Blood. 2015 Jan 8;125(2):211-2. doi: 10.1182/blood-2014-10-606582. PMID: 25573966. 10: Liu TM, Ling Y, Woyach JA, Beckwith K, Yeh YY, Hertlein E, Zhang X, Lehman A, Awan F, Jones JA, Andritsos LA, Maddocks K, MacMurray J, Salunke SB, Chen CS, Phelps MA, Byrd JC, Johnson AJ. OSU-T315: a novel targeted therapeutic that antagonizes AKT membrane localization and activation of chronic lymphocytic leukemia cells. Blood. 2015 Jan 8;125(2):284-95. doi: 10.1182/blood-2014-06-583518. Epub 2014 Oct 7. PMID: 25293770; PMCID: PMC4287637. 11: Lee SL, Hsu EC, Chou CC, Chuang HC, Bai LY, Kulp SK, Chen CS. Identification and characterization of a novel integrin-linked kinase inhibitor. J Med Chem. 2011 Sep 22;54(18):6364-74. doi: 10.1021/jm2007744. Epub 2011 Aug 24. PMID: 21823616; PMCID: PMC3182772.

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