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MedKoo Cat#: 562225 | Name: JR-AB2-011
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Description:

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

JR-AB2-011 is a potent and selective inhibitor of mTORC2 kinase activity. It markedly reduces mTORC2 signaling and IC50 while enhancing apoptotic levels in GBM cells. Note: JR-AB2-011 when published, the structure was CAS#329182-61-8. The same author corrected the structure in https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0212160. The new structure has CAS#2411853-34-2

Chemical Structure

JR-AB2-011
JR-AB2-011
CAS#2411853-34-2

Theoretical Analysis

MedKoo Cat#: 562225

Name: JR-AB2-011

CAS#: 2411853-34-2

Chemical Formula: C17H14Cl2FN3OS

Exact Mass: 397.0219

Molecular Weight: 398.28

Elemental Analysis: C, 51.27; H, 3.54; Cl, 17.80; F, 4.77; N, 10.55; O, 4.02; S, 8.05

Price and Availability

Size Price Availability Quantity
25mg USD 750.00 2 Weeks
100mg USD 1,950.00 2 Weeks
1g USD 5,650.00 2 Weeks
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Related CAS #
2411853-34-2 329182-61-8 (wrong)
Synonym
JR-AB2-011; JR AB-2-011; jb-AB 2-011; JRAB2011; JRAB-2011; JRAB 2011;
IUPAC/Chemical Name
(Z)-N-(3,4-dichlorophenyl)-2-((4-fluorophenyl)imino)-5-methylthiazolidine-3-carboxamide
InChi Key
TWTNZYABDOSOSR-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H14Cl2FN3OS/c1-10-9-21-17(25-10)23(13-5-2-11(20)3-6-13)16(24)22-12-4-7-14(18)15(19)8-12/h2-8,10H,9H2,1H3,(H,22,24)
SMILES Code
ClC1=C(Cl)C=C(NC(N2/C(SC(C)C2)=N/C3=CC=C(F)C=C3)=O)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
>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
https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0212160
Product Data
Product Data
Instruction
View handling instruction
Biological target:
JR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM).
In vitro activity:
Cell viability of all human melanoma cell lines was significantly reduced in a dose-dependent manner after exposure to 100 µM JR-AB2-011 for 48 h (MelJu, 70%, p = 0.017; MelJuso, 88%, p = 0.1; MelIm, 52%, p < 0.001) whereas murine melanoma cells were significantly affected by 10 µM JR-AB2-011 (B16, 63%, p = 0.04) (Figure 1A). Reference: Int J Mol Sci. 2020 Dec 22;22(1):30. https://pubmed.ncbi.nlm.nih.gov/33375117/
In vivo activity:
Mice were subcutaneously implanted with tumor cells and when tumors were palpable (~200 mm3), mice were randomized into treatment groups receiving vehicle, JR-AB2-011 (4 mg/kg/d) and JR-AB2-011 (20 mg/kg/d). As shown in Fig 6A, mice receiving JR-AB2-011 at either dosing regimen displayed marked inhibition of tumor growth rate (JR-AB2-011 at 4 mg/kg/d; 74% inhibition at end of dosing period; tumor growth delay 10.0 days; JR-AB2-011 at 20 mg/kg/d; 80% inhibition at end of dosing period; tumor growth delay 12.0 days) as compared to mice receiving vehicle alone. Consistent with the effects on xenograft growth, overall survival of mice at either JR-AB2-011 dosing regimen was significantly extended relative to vehicle treated mice. Reference: PLoS One. 2017 Apr 28;12(4):e0176599. https://pubmed.ncbi.nlm.nih.gov/28453552/
Solvent mg/mL mM
Solubility
Soluble in DMSO 0.0 100.00
Ethanol 3.0 7.53
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 398.28 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. Guenzle J, Akasaka H, Joechle K, Reichardt W, Venkatasamy A, Hoeppner J, Hellerbrand C, Fichtner-Feigl S, Lang SA. Pharmacological Inhibition of mTORC2 Reduces Migration and Metastasis in Melanoma. Int J Mol Sci. 2020 Dec 22;22(1):30. doi: 10.3390/ijms22010030. PMID: 33375117; PMCID: PMC7792954. 2. Benavides-Serrato A, Lee J, Holmes B, Landon KA, Bashir T, Jung ME, Lichtenstein A, Gera J. Specific blockade of Rictor-mTOR association inhibits mTORC2 activity and is cytotoxic in glioblastoma. PLoS One. 2017 Apr 28;12(4):e0176599. doi: 10.1371/journal.pone.0176599. Erratum in: PLoS One. 2019 Feb 6;14(2):e0212160. PMID: 28453552; PMCID: PMC5409528.
In vitro protocol:
1. Guenzle J, Akasaka H, Joechle K, Reichardt W, Venkatasamy A, Hoeppner J, Hellerbrand C, Fichtner-Feigl S, Lang SA. Pharmacological Inhibition of mTORC2 Reduces Migration and Metastasis in Melanoma. Int J Mol Sci. 2020 Dec 22;22(1):30. doi: 10.3390/ijms22010030. PMID: 33375117; PMCID: PMC7792954. 2. Benavides-Serrato A, Lee J, Holmes B, Landon KA, Bashir T, Jung ME, Lichtenstein A, Gera J. Specific blockade of Rictor-mTOR association inhibits mTORC2 activity and is cytotoxic in glioblastoma. PLoS One. 2017 Apr 28;12(4):e0176599. doi: 10.1371/journal.pone.0176599. Erratum in: PLoS One. 2019 Feb 6;14(2):e0212160. PMID: 28453552; PMCID: PMC5409528.
In vivo protocol:
1. Guenzle J, Akasaka H, Joechle K, Reichardt W, Venkatasamy A, Hoeppner J, Hellerbrand C, Fichtner-Feigl S, Lang SA. Pharmacological Inhibition of mTORC2 Reduces Migration and Metastasis in Melanoma. Int J Mol Sci. 2020 Dec 22;22(1):30. doi: 10.3390/ijms22010030. PMID: 33375117; PMCID: PMC7792954. 2. Benavides-Serrato A, Lee J, Holmes B, Landon KA, Bashir T, Jung ME, Lichtenstein A, Gera J. Specific blockade of Rictor-mTOR association inhibits mTORC2 activity and is cytotoxic in glioblastoma. PLoS One. 2017 Apr 28;12(4):e0176599. doi: 10.1371/journal.pone.0176599. Erratum in: PLoS One. 2019 Feb 6;14(2):e0212160. PMID: 28453552; PMCID: PMC5409528.
1: Benavides-Serrato A, Lee J, Holmes B, Landon KA, Bashir T, Jung ME, Lichtenstein A, Gera J. Specific blockade of Rictor-mTOR association inhibits mTORC2 activity and is cytotoxic in glioblastoma. PLoS One. 2017 Apr 28;12(4):e0176599. doi: 10.1371/journal.pone.0176599. eCollection 2017. PubMed PMID: 28453552; PubMed Central PMCID: PMC5409528.