WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H558220
CAS#: 1513879-18-9
Description: KAI407 is a potent non-8-aminoquinoline compound that kills Plasmodium cynomolgi early dormant liver stage parasites in vitro. KAI407 showed an activity profile similar to that of primaquine (PQ), efficiently killing the earliest stages of the parasites that become either primary hepatic schizonts or hypnozoites (50% inhibitory concentration [IC50] for hypnozoites, KAI407, 0.69 μM, and PQ, 0.84 μM; for developing liver stages, KAI407, 0.64 μM, and PQ, 0.37 μM). KAI407 may represent a new compound class for P. vivax malaria prophylaxis and potentially a radical cure.
Hodoodo Cat#: H558220
Name: KAI-407
CAS#: 1513879-18-9
Chemical Formula: C22H14F3N5O
Exact Mass: 421.12
Molecular Weight: 421.383
Elemental Analysis: C, 62.71; H, 3.35; F, 13.53; N, 16.62; O, 3.80
Synonym: KAI-407; KAI 407; KAI407.
IUPAC/Chemical Name: N-(4-cyanophenyl)-N-methyl-3-(4-(trifluoromethyl)phenyl)imidazo[1,2-a]pyrazine-6-carboxamide
InChi Key: XAZOWMVYGFASLH-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H14F3N5O/c1-29(17-8-2-14(10-26)3-9-17)21(31)18-13-30-19(11-28-20(30)12-27-18)15-4-6-16(7-5-15)22(23,24)25/h2-9,11-13H,1H3
SMILES Code: O=C(C1=CN2C(C=N1)=NC=C2C3=CC=C(C(F)(F)F)C=C3)N(C4=CC=C(C#N)C=C4)C
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, 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).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 421.38 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: |
1: Zou B, Nagle A, Chatterjee AK, Leong SY, Tan LJ, Sim WL, Mishra P, Guntapalli
P, Tully DC, Lakshminarayana SB, Lim CS, Tan YC, Abas SN, Bodenreider C, Kuhen
KL, Gagaring K, Borboa R, Chang J, Li C, Hollenbeck T, Tuntland T, Zeeman AM,
Kocken CH, McNamara C, Kato N, Winzeler EA, Yeung BK, Diagana TT, Smith PW,
Roland J. Lead optimization of imidazopyrazines: a new class of antimalarial with
activity on Plasmodium liver stages. ACS Med Chem Lett. 2014 Jul 6;5(8):947-50.
doi: 10.1021/ml500244m. eCollection 2014 Aug 14. PubMed PMID: 25147620; PubMed
Central PMCID: PMC4137381.
2: Zeeman AM, van Amsterdam SM, McNamara CW, Voorberg-van der Wel A, Klooster EJ,
van den Berg A, Remarque EJ, Plouffe DM, van Gemert GJ, Luty A, Sauerwein R,
Gagaring K, Borboa R, Chen Z, Kuhen K, Glynne RJ, Chatterjee AK, Nagle A, Roland
J, Winzeler EA, Leroy D, Campo B, Diagana TT, Yeung BK, Thomas AW, Kocken CH.
KAI407, a potent non-8-aminoquinoline compound that kills Plasmodium cynomolgi
early dormant liver stage parasites in vitro. Antimicrob Agents Chemother.
2014;58(3):1586-95. doi: 10.1128/AAC.01927-13. Epub 2013 Dec 23. PubMed PMID:
24366744; PubMed Central PMCID: PMC3957848.