KAF156

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MedKoo CAT#: 565769

CAS#: 1261113-96-5

Description: KAF156 (Ganaplacide) is a drug in development by Novartis for the purpose of treating malaria. It belongs to the class of the imidazolopiperazines. It has shown activity against the Plasmodium falciparum and Plasmodium vivax forms of the malaria parasite. The antimalarial activity of the imidazolopiperazine compound class was initially discovered through a series of sensitive phenotypic antimalarial screens that were developed and run in 2007 and 2008 by a group of biologists working at the Genomics Institute of the Novartis Research Foundation and the Scripps Research Institute.


Chemical Structure

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KAF156
CAS# 1261113-96-5

Theoretical Analysis

MedKoo Cat#: 565769
Name: KAF156
CAS#: 1261113-96-5
Chemical Formula: C22H23F2N5O
Exact Mass: 411.19
Molecular Weight: 411.457
Elemental Analysis: C, 64.22; H, 5.63; F, 9.23; N, 17.02; O, 3.89

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: KAF156; KAF 156; KAF-156

IUPAC/Chemical Name: 2-Amino-1-[3-(4-fluoroanilino)-2-(4-fluorophenyl)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7-yl]ethanone

InChi Key: BUPRVECGWBHCQV-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H23F2N5O/c1-22(2)21-27-19(14-3-5-15(23)6-4-14)20(26-17-9-7-16(24)8-10-17)28(21)11-12-29(22)18(30)13-25/h3-10,26H,11-13,25H2,1-2H3

SMILES Code: CC1(C)C2=NC(C3=CC=C(F)C=C3)=C(NC4=CC=C(F)C=C4)N2CCN1C(CN)=O

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 411.46 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:
In vitro protocol:
In vivo protocol:

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1: White NJ, Duong TT, Uthaisin C, Nosten F, Phyo AP, Hanboonkunupakarn B, Pukrittayakamee S, Jittamala P, Chuthasmit K, Cheung MS, Feng Y, Li R, Magnusson B, Sultan M, Wieser D, Xun X, Zhao R, Diagana TT, Pertel P, Leong FJ. Antimalarial Activity of KAF156 in Falciparum and Vivax Malaria. N Engl J Med. 2016 Sep 22;375(12):1152-60. doi: 10.1056/NEJMoa1602250. PubMed PMID: 27653565; PubMed Central PMCID: PMC5142602.

2: Huskey SE, Forseth RR, Li H, Jian Z, Catoire A, Zhang J, Ray T, He H, Flarakos J, Mangold JB. Utilization of Stable Isotope Labeling to Facilitate the Identification of Polar Metabolites of KAF156, an Antimalarial Agent. Drug Metab Dispos. 2016 Oct;44(10):1697-708. doi: 10.1124/dmd.116.072108. Epub 2016 Aug 2. PubMed PMID: 27486238.

3: Leong FJ, Jain JP, Feng Y, Goswami B, Stein DS. A phase 1 evaluation of the pharmacokinetic/pharmacodynamic interaction of the anti-malarial agents KAF156 and piperaquine. Malar J. 2018 Jan 5;17(1):7. doi: 10.1186/s12936-017-2162-8. PubMed PMID: 29304859; PubMed Central PMCID: PMC5756412.

4: Kuhen KL, Chatterjee AK, Rottmann M, Gagaring K, Borboa R, Buenviaje J, Chen Z, Francek C, Wu T, Nagle A, Barnes SW, Plouffe D, Lee MC, Fidock DA, Graumans W, van de Vegte-Bolmer M, van Gemert GJ, Wirjanata G, Sebayang B, Marfurt J, Russell B, Suwanarusk R, Price RN, Nosten F, Tungtaeng A, Gettayacamin M, Sattabongkot J, Taylor J, Walker JR, Tully D, Patra KP, Flannery EL, Vinetz JM, Renia L, Sauerwein RW, Winzeler EA, Glynne RJ, Diagana TT. KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission. Antimicrob Agents Chemother. 2014 Sep;58(9):5060-7. doi: 10.1128/AAC.02727-13. Epub 2014 Jun 9. PubMed PMID: 24913172; PubMed Central PMCID: PMC4135840.

5: Koller R, Mombo-Ngoma G, Grobusch MP. The early preclinical and clinical development of ganaplacide (KAF156), a novel antimalarial compound. Expert Opin Investig Drugs. 2018 Oct;27(10):803-810. doi: 10.1080/13543784.2018.1524871. Epub 2018 Sep 25. Review. PubMed PMID: 30223692.

6: Ashley EA, Phyo AP. Drugs in Development for Malaria. Drugs. 2018 Jun;78(9):861-879. doi: 10.1007/s40265-018-0911-9. Review. PubMed PMID: 29802605; PubMed Central PMCID: PMC6013505.

7: Leong FJ, Zhao R, Zeng S, Magnusson B, Diagana TT, Pertel P. A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel Imidazolopiperazine KAF156 to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers. Antimicrob Agents Chemother. 2014 Nov;58(11):6437-43. doi: 10.1128/AAC.03478-14. Epub 2014 Aug 18. PubMed PMID: 25136017; PubMed Central PMCID: PMC4249437.

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9: Held J, Jeyaraj S, Kreidenweiss A. Antimalarial compounds in Phase II clinical development. Expert Opin Investig Drugs. 2015 Mar;24(3):363-82. doi: 10.1517/13543784.2015.1000483. Epub 2015 Jan 7. Review. PubMed PMID: 25563531.

10: Magistrado PA, Corey VC, Lukens AK, LaMonte G, Sasaki E, Meister S, Wree M, Winzeler E, Wirth DF. Plasmodium falciparum Cyclic Amine Resistance Locus (PfCARL), a Resistance Mechanism for Two Distinct Compound Classes. ACS Infect Dis. 2016 Nov 11;2(11):816-826. Epub 2016 Apr 7. PubMed PMID: 27933786; PubMed Central PMCID: PMC5109296.

11: Diagana TT. Supporting malaria elimination with 21st century antimalarial agent drug discovery. Drug Discov Today. 2015 Oct;20(10):1265-70. doi: 10.1016/j.drudis.2015.06.009. Epub 2015 Jun 21. Review. PubMed PMID: 26103616.

12: Mathews ES, Odom John AR. Tackling resistance: emerging antimalarials and new parasite targets in the era of elimination. F1000Res. 2018 Aug 1;7. pii: F1000 Faculty Rev-1170. doi: 10.12688/f1000research.14874.1. eCollection 2018. Review. PubMed PMID: 30135714; PubMed Central PMCID: PMC6073090.

13: Mischlinger J, Agnandji ST, Ramharter M. Single dose treatment of malaria - current status and perspectives. Expert Rev Anti Infect Ther. 2016 Jul;14(7):669-78. doi: 10.1080/14787210.2016.1192462. Epub 2016 Jun 7. Review. PubMed PMID: 27254098.

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15: Rossier J, Nasiri Sovari S, Pavic A, Vojnovic S, Stringer T, Bättig S, Smith GS, Nikodinovic-Runic J, Zobi F. Antiplasmodial Activity and In Vivo Bio-Distribution of Chloroquine Molecules Released with a 4-(4-Ethynylphenyl)-Triazole Moiety from Organometallo-Cobalamins. Molecules. 2019 Jun 21;24(12). pii: E2310. doi: 10.3390/molecules24122310. PubMed PMID: 31234469.