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

MedKoo CAT#: 591336

CAS#: 1047644-62-1 (free base)

Description: Afuresertib, also known as GSK-2110183 or GSK-2110183C, is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Afuresertib binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis


Price and Availability

Size
Price

10mg
USD 345
Size
Price

100mg
USD 1250
Size
Price

Afuresertib free base, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 591336
Name: Afuresertib free base
CAS#: 1047644-62-1 (free base)
Chemical Formula: C18H17Cl2FN4OS
Exact Mass: 426.0784
Molecular Weight: 427.32
Elemental Analysis: C, 50.59; H, 4.01; Cl, 16.59; F, 4.45; N, 13.11; O, 3.74; S, 7.50


Related CAS #: 1047634-63-8   1047645-82-8 (HCl)   1047644-62-1 (free base)    

Synonym: GSK2110183; GSK 2110183; GSK-2110183; GSK2110183C; GSK 2110183C; GSK2110183C; Afuresertib free base;

IUPAC/Chemical Name: 2-Thiophenecarboxamide, N-((1S)-2-amino-1-((3-fluorophenyl)methyl)ethyl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-

InChi Key: AFJRDFWMXUECEW-LBPRGKRZSA-N

InChi Code: InChI=1S/C18H17Cl2FN4OS/c1-25-16(14(19)9-23-25)13-7-15(27-17(13)20)18(26)24-12(8-22)6-10-3-2-4-11(21)5-10/h2-5,7,9,12H,6,8,22H2,1H3,(H,24,26)/t12-/m0/s1

SMILES Code: O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[C@@H](CC3=CC=CC(F)=C3)CN


Technical Data

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).

Harmonized System Code:
293490


References

1: Ni H, Shirazi F, Baladandayuthapani V, Lin H, Kuiatse I, Wang H, Jones RJ, Berkova Z, Hitoshi Y, Ansell SM, Treon SP, Thomas SK, Lee HC, Wang Z, Davis RE, Orlowski RZ. Targeting Myddosome Signaling in Waldenström's Macroglobulinemia with the Interleukin-1 Receptor-Associated Kinase 1/4 Inhibitor R191. Clin Cancer Res. 2018 Aug 20. doi: 10.1158/1078-0432.CCR-17-3265. [Epub ahead of print] PubMed PMID: 30126942.

2: Kinoshita S, Ri M, Kanamori T, Aoki S, Yoshida T, Narita T, Totani H, Ito A, Kusumoto S, Ishida T, Komatsu H, Iida S. Potent antitumor effect of combination therapy with sub-optimal doses of Akt inhibitors and pomalidomide plus dexamethasone in multiple myeloma. Oncol Lett. 2018 Jun;15(6):9450-9456. doi: 10.3892/ol.2018.8501. Epub 2018 Apr 16. PubMed PMID: 29928335; PubMed Central PMCID: PMC6004690.

3: Chen CI, Paul H, Le LW, Wei EN, Snitzler S, Wang T, Levina O, Kakar S, Lau A, Queau M, Johnston JB, Smith DA, Trudel S. A phase 2 study of ofatumumab (Arzerra(®)) in combination with a pan-AKT inhibitor (afuresertib) in previously treated patients with chronic lymphocytic leukemia (CLL). Leuk Lymphoma. 2018 Jun 19:1-9. doi: 10.1080/10428194.2018.1468892. [Epub ahead of print] PubMed PMID: 29916761.

4: Yamaji M, Ota A, Wahiduzzaman M, Karnan S, Hyodo T, Konishi H, Tsuzuki S, Hosokawa Y, Haniuda M. Novel ATP-competitive Akt inhibitor afuresertib suppresses the proliferation of malignant pleural mesothelioma cells. Cancer Med. 2017 Nov;6(11):2646-2659. doi: 10.1002/cam4.1179. Epub 2017 Sep 27. PubMed PMID: 28960945; PubMed Central PMCID: PMC5673922.

5: Arceci RJ, Allen CE, Dunkel IJ, Jacobsen E, Whitlock J, Vassallo R, Morris SR, Portnoy A, Reedy BA, Smith DA, Noble R, Murnane A, Cornfeld M, Rodriguez-Galindo C, Heaney ML, McClain K, Vaiselbuh S. A phase IIa study of afuresertib, an oral pan-AKT inhibitor, in patients with Langerhans cell histiocytosis. Pediatr Blood Cancer. 2017 May;64(5). doi: 10.1002/pbc.26325. Epub 2016 Nov 2. PubMed PMID: 27804235.

6: Naymagon L, Abdul-Hay M. Novel agents in the treatment of multiple myeloma: a review about the future. J Hematol Oncol. 2016 Jun 30;9(1):52. doi: 10.1186/s13045-016-0282-1. Review. PubMed PMID: 27363832; PubMed Central PMCID: PMC4929712.

7: Tolcher AW, Patnaik A, Papadopoulos KP, Rasco DW, Becerra CR, Allred AJ, Orford K, Aktan G, Ferron-Brady G, Ibrahim N, Gauvin J, Motwani M, Cornfeld M. Phase I study of the MEK inhibitor trametinib in combination with the AKT inhibitor afuresertib in patients with solid tumors and multiple myeloma. Cancer Chemother Pharmacol. 2015 Jan;75(1):183-9. doi: 10.1007/s00280-014-2615-5. Epub 2014 Nov 25. PubMed PMID: 25417902.

8: Leleu X. A key to the quest? Blood. 2014 Oct 2;124(14):2162-3. doi: 10.1182/blood-2014-08-593822. PubMed PMID: 25278563.

9: Spencer A, Yoon SS, Harrison SJ, Morris SR, Smith DA, Brigandi RA, Gauvin J, Kumar R, Opalinska JB, Chen C. The novel AKT inhibitor afuresertib shows favorable safety, pharmacokinetics, and clinical activity in multiple myeloma. Blood. 2014 Oct 2;124(14):2190-5. doi: 10.1182/blood-2014-03-559963. Epub 2014 Jul 29. PubMed PMID: 25075128; PubMed Central PMCID: PMC4229853.

10: Keane NA, Glavey SV, Krawczyk J, O'Dwyer M. AKT as a therapeutic target in multiple myeloma. Expert Opin Ther Targets. 2014 Aug;18(8):897-915. doi: 10.1517/14728222.2014.924507. Epub 2014 Jun 6. Review. PubMed PMID: 24905897.