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MedKoo Cat#: 462405 | Name: GSK 525768A
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Description:

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

GSK 525768A is the inactive enantiomer of GSK525762A and has no activity towards BET.

Chemical Structure

GSK 525768A
GSK 525768A
CAS#1260530-25-3

Theoretical Analysis

MedKoo Cat#: 462405

Name: GSK 525768A

CAS#: 1260530-25-3

Chemical Formula: C22H22ClN5O2

Exact Mass: 423.1462

Molecular Weight: 423.90

Elemental Analysis: C, 62.34; H, 5.23; Cl, 8.36; N, 16.52; O, 7.55

Price and Availability

Size Price Availability Quantity
5mg USD 750.00 2 Weeks
10mg USD 1,250.00 2 Weeks
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Related CAS #
No Data
Synonym
GSK 525768A; GSK525768A; GSK-525768A
IUPAC/Chemical Name
2-((4R)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide
InChi Key
AAAQFGUYHFJNHI-GOSISDBHSA-N
InChi Code
InChI=1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m1/s1
SMILES Code
ClC1=CC=C(C2=N[C@H](CC(NCC)=O)C3=NN=C(C)N3C4=C2C=C(OC)C=C4)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
>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
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
GSK 525768A is the inactive enantiomer of GSK525762A.
In vitro activity:
The effects of bromodomain-containing protein 4 (BRD4) inhibitor GSK525762A on the proliferation and apoptosis of primary common B-cell acute lymphoblastic leukemia (common B-ALL) cells were investigated. GSK525762A inhibited the proliferation of leukemia cells in a dose-dependent manner, the median value of IC50 was 256.25 (90.64-1 378.39)nmol/L. GSK525762A promoted cells apoptosis of B-ALL leukemia cells in a dose-dependent manner, the median apoptosis rates respectively were 45.17%(9.38%- 70.91%), 66.02% (24.36%-96.34%) and 89.29% (39.29%-99.37%) after treated by 500, 1 000 and 2 500 nmol/L GSK525762A. GSK525762A had a similar effect on Ph⁺ ALL and Ph⁻ B-ALL, but the effect of proliferation inhibition and apoptosis enhancement on Ph+ B-ALL was weaker than that on Ph⁻ B-ALL. Compared with vehicle control group, the levels of c-MYC, Bcl-2 and CDK6 transcripts in leukemic cells were reduced after treatment for 24 h and 48 h by 1 000 nmol/L GSK525762A, and there were no significant differences in the downregulation of c-MYC and CDK6 mRNA between Ph⁺ and Ph⁻ B-ALL; however, the inhibitory effect on Bcl-2 transcription was weaker in Ph⁺ B-ALL cells than that in Ph⁻ B-ALL cells. Moreover, c-MYC, Bcl-2 and CDK6 protein levels decreased in GSK525762A treated group. Reference: Zhonghua Xue Ye Xue Za Zhi. 2015 Jul;36(7):563-9. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7342640/
In vivo activity:
In Panc-1 tumor-bearing mice, GEM (Gemcitabine) and I-BET762 decreased the tumor weight and volume. The combination of GEM and I-BET762 triggered a remarkable decline in tumor weight and volume compared with that of either agent alone (Fig. 6A). TUNEL and Ki67 assays indicated that I-BET762 and GEM induced less apoptosis when used alone than did the combination treatment (Fig. 6B and C). In contrast, compared with the parental tumors, Bim-KD tumors showed noticeably weaker growth suppression in response to the combination therapy (Fig. 6A–C). Reference: Sci Rep. 2018 May 25;8(1):8102. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5970200/
Solvent mg/mL mM
Solubility
DMSO 100.0 235.90
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 423.90 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. Ma S, Chen C, Zhu J, Li Y, Wang X, Song X, Cao J, Xu K. [In vitro study of BRD4 inhibitor GSK525762A against primary adult common B-cell acute lymphoblastic leukemia cells in vitro]. Zhonghua Xue Ye Xue Za Zhi. 2015 Jul;36(7):563-9. Chinese. doi: 10.3760/cma.j.issn.0253-2727.2015.07.007. PMID: 26304078; PMCID: PMC7342640. 2. Wang X, Qi N, Ma S, Yan ZL, Wu QY, Wang L, Chen C, Xu KL. [Effect of BRD4 Inhibitor GSK525762A on Proliferation and Apoptosis of SUP-B15 Cells In Vitro and Its Possible Mechanism]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2016 Dec;24(6):1654- 1658. Chinese. doi: 10.7534/j.issn.1009-2137.2016.06.008. PMID: 28024472. 3. Xie F, Huang M, Lin X, Liu C, Liu Z, Meng F, Wang C, Huang Q. The BET inhibitor I-BET762 inhibits pancreatic ductal adenocarcinoma cell proliferation and enhances the therapeutic effect of gemcitabine. Sci Rep. 2018 May 25;8(1):8102. doi: 10.1038/s41598-018-26496-0. PMID: 29802402; PMCID: PMC5970200.
In vitro protocol:
1. Ma S, Chen C, Zhu J, Li Y, Wang X, Song X, Cao J, Xu K. [In vitro study of BRD4 inhibitor GSK525762A against primary adult common B-cell acute lymphoblastic leukemia cells in vitro]. Zhonghua Xue Ye Xue Za Zhi. 2015 Jul;36(7):563-9. Chinese. doi: 10.3760/cma.j.issn.0253-2727.2015.07.007. PMID: 26304078; PMCID: PMC7342640. 2. Wang X, Qi N, Ma S, Yan ZL, Wu QY, Wang L, Chen C, Xu KL. [Effect of BRD4 Inhibitor GSK525762A on Proliferation and Apoptosis of SUP-B15 Cells In Vitro and Its Possible Mechanism]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2016 Dec;24(6):1654- 1658. Chinese. doi: 10.7534/j.issn.1009-2137.2016.06.008. PMID: 28024472.
In vivo protocol:
1. Xie F, Huang M, Lin X, Liu C, Liu Z, Meng F, Wang C, Huang Q. The BET inhibitor I-BET762 inhibits pancreatic ductal adenocarcinoma cell proliferation and enhances the therapeutic effect of gemcitabine. Sci Rep. 2018 May 25;8(1):8102. doi: 10.1038/s41598-018-26496-0. PMID: 29802402; PMCID: PMC5970200.
1: Nicodeme E, Jeffrey KL, Schaefer U, et al. Suppression of inflammation by a synthetic histone mimic. Nature. 2010;468(7327):1119-1123. doi:10.1038/nature09589 2: Filippakopoulos P, Knapp S. Targeting bromodomains: epigenetic readers of lysine acetylation. Nat Rev Drug Discov. 2014;13(5):337-356. doi:10.1038/nrd4286