OXA-01 | CAS#936889-68-8 | TORC inhibitor

OXA-01
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407427

CAS#: 936889-68-8

Description: OXA-01 is an inhibitor of both mTORC1 and mTORC2 (IC50s = 11 and 29 nM, respectively). OXA-01 targeted both mTORC1 and mTORC2 signaling in vitro and in vivo. OXA-01 reduced VEGF production in tumors in a manner associated with decreased vessel sprouting but little vascular regression.

Chemical Structure

OXA-01

CAS# 936889-68-8

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 407427
Name: OXA-01
CAS#: 936889-68-8
Chemical Formula: C21H20ClN5O2
Exact Mass: 409.13
Molecular Weight: 409.874
Elemental Analysis: C, 61.54; H, 4.92; Cl, 8.65; N, 17.09; O, 7.81

Price and Availability

Size	Price	Availability
5mg	USD 290	2 Weeks
10mg	USD 500	2 Weeks
25mg	USD 900	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: OXA-01; OXA01; OXA 01.

IUPAC/Chemical Name: trans-4-[8-amino-1-(7-chloro-1H-indol-2-yl)imidazo[1,5-a]pyrazin-3-yl]-cyclohexanecarboxylic acid

InChi Key: UXCAKZGNKOZXBM-HAQNSBGRSA-N

InChi Code: InChI=1S/C21H20ClN5O2/c22-14-3-1-2-13-10-15(25-16(13)14)17-18-19(23)24-8-9-27(18)20(26-17)11-4-6-12(7-5-11)21(28)29/h1-3,8-12,25H,4-7H2,(H2,23,24)(H,28,29)/t11-,12-

SMILES Code: O=C([C@H]1CC[C@H](C2=NC(C(N3)=CC4=C3C(Cl)=CC=C4)=C5C(N)=NC=CN52)CC1)O

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: >2 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:

Product Data:

Product Data

Instruction:

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Biological target:	OXA-01 is a potent mTORC1 and mTORC2 inhibitor, with IC50 values of 29 nM and 7 nM.
In vitro activity:	Effects of OXA-01, OSI-027, and rapamycin on mTORC1 and mTORC2 signaling were compared in vitro. OXA-01 or OSI-027, but not rapamycin, dose-dependently attenuated Akt phosphorylation at the mTORC2-specific Ser473 site and the downstream substrate of Akt, PRAS40 (Supplemental Figure 1A). OXA-01 and OSI-027 inhibited 4E-BP1 phosphorylation at Ser37/46, which are typically rapamycin insensitive. Reference: Cancer Res. 2011 Mar 1;71(5):1573-83. https://pubmed.ncbi.nlm.nih.gov/21363918/
In vivo activity:	Consistent with their inhibition of mTORC1 and mTORC2, both OSI-027 (Figure 2C) and OXA-01 (Figure 2D) slowed tumor growth more than did rapamycin. As indicated by reduced tumor growth in mouse xenograft models, OXA-01 treatment decreased cellular proliferation determined by phospho-histone H3 (Figure 3C) and increased apoptosis measured by activated-caspase-3 (Figure 3D). Reference: Cancer Res. 2011 Mar 1;71(5):1573-83. https://pubmed.ncbi.nlm.nih.gov/21363918/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	1.0	2.44
	DMSO	3.0	7.32
	DMSO:PBS (pH 7.2) (1:3)	0.3	0.61

Preparing Stock Solutions

The following data is based on the product molecular weight 409.87 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:	Falcon BL, Barr S, Gokhale PC, Chou J, Fogarty J, Depeille P, Miglarese M, Epstein DM, McDonald DM. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. Cancer Res. 2011 Mar 1;71(5):1573-83. doi: 10.1158/0008-5472.CAN-10-3126. PMID: 21363918; PMCID: PMC3077087.
In vitro protocol:	Falcon BL, Barr S, Gokhale PC, Chou J, Fogarty J, Depeille P, Miglarese M, Epstein DM, McDonald DM. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. Cancer Res. 2011 Mar 1;71(5):1573-83. doi: 10.1158/0008-5472.CAN-10-3126. PMID: 21363918; PMCID: PMC3077087.
In vivo protocol:	Falcon BL, Barr S, Gokhale PC, Chou J, Fogarty J, Depeille P, Miglarese M, Epstein DM, McDonald DM. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. Cancer Res. 2011 Mar 1;71(5):1573-83. doi: 10.1158/0008-5472.CAN-10-3126. PMID: 21363918; PMCID: PMC3077087.

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1: Bhagwat SV, Gokhale PC, Crew AP, Cooke A, Yao Y, Mantis C, Kahler J, Workman
J, Bittner M, Dudkin L, Epstein DM, Gibson NW, Wild R, Arnold LD, Houghton PJ,
Pachter JA. Preclinical characterization of OSI-027, a potent and selective
inhibitor of mTORC1 and mTORC2: distinct from rapamycin. Mol Cancer Ther. 2011
Aug;10(8):1394-406. doi: 10.1158/1535-7163.MCT-10-1099. PubMed PMID: 21673091.

2: Falcon BL, Barr S, Gokhale PC, Chou J, Fogarty J, Depeille P, Miglarese M,
Epstein DM, McDonald DM. Reduced VEGF production, angiogenesis, and vascular
regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors.
Cancer Res. 2011 Mar 1;71(5):1573-83. doi: 10.1158/0008-5472.CAN-10-3126. PubMed
PMID: 21363918; PubMed Central PMCID: PMC3077087.

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