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

OSU-T315 (1,5-regioisomer)
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 564620

CAS#: 1333146-24-9

Description: 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)

CAS# 1333146-24-9

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 564620
Name: OSU-T315 (1,5-regioisomer)
CAS#: 1333146-24-9
Chemical Formula: C30H30F3N5O
Exact Mass: 533.24
Molecular Weight: 533.599
Elemental Analysis: C, 67.53; H, 5.67; F, 10.68; N, 13.13; O, 3.00

Price and Availability

Size	Price	Availability
5mg	USD 400	2 Weeks
10mg	USD 750	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	50.0	93.70

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.

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.

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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. eCollection 2018. PubMed PMID: 30276218; PubMed Central PMCID: PMC6157143.

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). pii: 1025. Epub 2016 Apr 21. PubMed PMID: 27642646; PubMed Central PMCID: PMC5024787.

3: Robak T, Smolewski P. Novel target to kill CLL. Blood. 2015 Jan 8;125(2):211-2. doi: 10.1182/blood-2014-10-606582. PubMed PMID: 25573966.

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. PubMed PMID: 25293770; PubMed Central PMCID: PMC4287637.

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