Afuresertib-F free base | CAS#| 1047634-63-8 | ATK inhibitor

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

MedKoo CAT#: 206994

CAS#: 1047634-63-8 (Afuresertib-F free base)

Description: Afuresertib-F is an analogue of Afuresertib with one more flurorine-atom compared to its parent drug Afuresertib. Afuresertib-F is an ATK inhibitor. Afuresertib, also known as GSK-2110183 or GSK-2110183C, is an cancer drug candidate under clinical trial.

Chemical Structure

Afuresertib-F free base

CAS# 1047634-63-8 (Afuresertib-F free base)

Instruction

Theoretical Analysis

MedKoo Cat#: 206994
Name: Afuresertib-F free base
CAS#: 1047634-63-8 (Afuresertib-F free base)
Chemical Formula: C18H16Cl2F2N4OS
Exact Mass: 444.04
Molecular Weight: 445.310
Elemental Analysis: C, 48.55; H, 3.62; Cl, 15.92; F, 8.53; N, 12.58; O, 3.59; S, 7.20

Price and Availability

Size	Price	Availability
1g	USD 3950	2-3 months
2g	USD 6950	2-3 months
5g	USD 11950	2-3 months
10g	USD 16950	2-3 months
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Afuresertib-F; GSK-2110183-analog; GSK2110183-analog; GSK 2110183-analog; Afuresertib-F free base

IUPAC/Chemical Name: N-[(2S)-1-Amino-3-(3,4-difluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)thiophene-2-carboxamide

InChi Key: AHDFWNJLFALBJP-JTQLQIEISA-N

InChi Code: InChI=1S/C18H16Cl2F2N4OS/c1-26-16(12(19)8-24-26)11-6-15(28-17(11)20)18(27)25-10(7-23)4-9-2-3-13(21)14(22)5-9/h2-3,5-6,8,10H,4,7,23H2,1H3,(H,25,27)/t10-/m0/s1

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

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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 445.31 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.

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:
In vitro protocol:
In vivo protocol:

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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.

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Afuresertib-F free base featured