GSK-923295
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206036

CAS#: 1088965-37-0

Description: GSK-923295, also known as GSK-923295A, is a novel antimitotic inhibitor of centromere-associated protein E (CENP-E) with potential anticancer activity. GSK923295A demonstrated significant antitumor activity against solid tumor models, inducing CRs in Ewing sarcoma, rhabdoid, and rhabdomyosarcoma xenografts. Clinical study showed that GSK923295 had dose-proportional pharmacokinetics and a low number of grade 3 or 4 adverse events. The observed incidence of myelosuppression and neuropathy was low. Further investigations may provide a more complete understanding of the potential for GSK923295 as an antiproliferative agent.


Chemical Structure

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GSK-923295
CAS# 1088965-37-0

Theoretical Analysis

MedKoo Cat#: 206036
Name: GSK-923295
CAS#: 1088965-37-0
Chemical Formula: C32H38ClN5O4
Exact Mass: 591.26123
Molecular Weight: 592.13
Elemental Analysis: C, 64.91; H, 6.47; Cl, 5.99; N, 11.83; O, 10.81

Size Price Shipping out time Quantity
5mg USD 150 Same day
10mg USD 250 Same day
25mg USD 450 Same day
50mg USD 750 Same day
100mg USD 1150 Same day
200mg USD 1850 Same day
500mg USD 2650 2 weeks
1g USD 3650 2 weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-02. Prices are subject to change without notice.

GSK-923295, purity > 97%, is in stock. The same day shipping out after order is received.

Synonym: GSK923295; GSK 923295; GSK-923295; GSK-923295A; GSK923295A; GSK 923295A.

IUPAC/Chemical Name: 3-Chloro-N-{(1S)-2-[(N,N-dimethylglycyl)amino]-1-[(4-{8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl}phenyl)methyl]ethyl}-4-[(1-methylethyl)oxy]benzamide

InChi Key: WHMXDBPHBVLYRC-OFVILXPXSA-N

InChi Code: InChI=1S/C32H38ClN5O4/c1-20(2)42-29-13-12-24(16-27(29)33)32(41)35-25(17-34-30(40)19-37(4)5)15-22-8-10-23(11-9-22)28-18-38-14-6-7-26(21(3)39)31(38)36-28/h6-14,16,18,20-21,25,39H,15,17,19H2,1-5H3,(H,34,40)(H,35,41)/t21-,25-/m0/s1

SMILES Code: O=C(N[C@@H](CC1=CC=C(C2=CN3C=CC=C([C@@H](O)C)C3=N2)C=C1)CNC(CN(C)C)=O)C4=CC=C(OC(C)C)C(Cl)=C4

Appearance:
Solid powder

Purity:
>97% (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, not in water

Shelf Life:
>5 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

Preparing Stock Solutions

The following data is based on the product molecular weight 592.13 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.

Select a batch to recalculate based on the batch molecular weight:
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

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1: Mayes PA, Degenhardt YY, Wood A, Toporovskya Y, Diskin SJ, Haglund E, Moy C, Wooster R, Maris JM. Mitogen-activated protein kinase (MEK/ERK) inhibition sensitizes cancer cells to centromere-associated protein E inhibition. Int J Cancer. 2013 Feb 1;132(3):E149-57. doi: 10.1002/ijc.27781. Epub 2012 Sep 28. PubMed PMID: 22948716.

2: Chung V, Heath EI, Schelman WR, Johnson BM, Kirby LC, Lynch KM, Botbyl JD, Lampkin TA, Holen KD. First-time-in-human study of GSK923295, a novel antimitotic inhibitor of centromere-associated protein E (CENP-E), in patients with refractory cancer. Cancer Chemother Pharmacol. 2012 Mar;69(3):733-41. doi: 10.1007/s00280-011-1756-z. Epub 2011 Oct 22. PubMed PMID: 22020315.

3: Lock RB, Carol H, Morton CL, Keir ST, Reynolds CP, Kang MH, Maris JM, Wozniak AW, Gorlick R, Kolb EA, Houghton PJ, Smith MA. Initial testing of the CENP-E inhibitor GSK923295A by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012 Jun;58(6):916-23. doi: 10.1002/pbc.23176. Epub 2011 May 16. PubMed PMID: 21584937; PubMed Central PMCID: PMC3163687.

4: Balamuth NJ, Wood A, Wang Q, Jagannathan J, Mayes P, Zhang Z, Chen Z, Rappaport E, Courtright J, Pawel B, Weber B, Wooster R, Sekyere EO, Marshall GM, Maris JM. Serial transcriptome analysis and cross-species integration identifies centromere-associated protein E as a novel neuroblastoma target. Cancer Res. 2010 Apr 1;70(7):2749-58. doi: 10.1158/0008-5472.CAN-09-3844. Epub 2010 Mar 16. PubMed PMID: 20233875; PubMed Central PMCID: PMC2848992.

5: Wood KW, Lad L, Luo L, Qian X, Knight SD, Nevins N, Brejc K, Sutton D, Gilmartin AG, Chua PR, Desai R, Schauer SP, McNulty DE, Annan RS, Belmont LD, Garcia C, Lee Y, Diamond MA, Faucette LF, Giardiniere M, Zhang S, Sun CM, Vidal JD, Lichtsteiner S, Cornwell WD, Greshock JD, Wooster RF, Finer JT, Copeland RA, Huang PS, Morgans DJ Jr, Dhanak D, Bergnes G, Sakowicz R, Jackson JR. Antitumor activity of an allosteric inhibitor of centromere-associated protein-E. Proc Natl Acad Sci U S A. 2010 Mar 30;107(13):5839-44. doi: 10.1073/pnas.0915068107. Epub 2010 Feb 18. PubMed PMID: 20167803; PubMed Central PMCID: PMC2851928.



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