Afuresertib HCl
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MedKoo CAT#: 205478

CAS#: 1047645-82-8 (HCl); 1047644-62-1 (free base).

Description: Afuresertib, also known as GSK2110183, is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GSK2110183 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 and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.


Price and Availability

Size
Price

10mg
USD 90
100mg
USD 450
1g
USD 2350
10g
USD 6950
Size
Price

25mg
USD 150
200mg
USD 650
2g
USD 3750
20g
USD 11750
Size
Price

50mg
USD 250
500mg
USD 1350
5g
USD 4950
50g
Ask price

Afuresertib HCl (GSK2110183 HCl), purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 200mg may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205478
Name: Afuresertib HCl
CAS#: 1047645-82-8 (HCl); 1047644-62-1 (free base).
Chemical Formula: C18H18Cl3FN4OS
Exact Mass:
Molecular Weight: 463.78
Elemental Analysis: C, 46.62; H, 3.91; Cl, 22.93; F, 4.10; N, 12.08; O, 3.45; S, 6.91


Synonym: GSK2110183; GSK 2110183; GSK-2110183; GSK2110183B; GSK 2110183B; GSK2110183B; Afuresertib.

IUPAC/Chemical Name: N-((S)-1-amino-3-(3-fluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide hydrochloride

InChi Key: YFQJOPFTGMHYNV-YDALLXLXSA-N

InChi Code: InChI=1S/C18H17Cl2FN4OS.ClH/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);1H/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.[H]Cl


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

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:
>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


Additional Information

Related:
1047645-82-8 (Afuresertib HCl)
1047644-62-1 (Afuresertib free base).


References

1: 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.

2: 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.

3: 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.

4: 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.