CRK12-IN-1
CRK12-IN-1 is a potent CRK12 inhibitor. CRK12-IN-1 is extremely potent against T.b. brucei and rapidly cytocidal, as well as equally potent against T. congolense and T. vivax (EC50 of 1.3 and 18 nM, respectively).
For research use only. We do not sell to patients.
- CAS No.: 1990479-14-5
- Formula: C20H26F2N4O3S2
- Molecular Weight:472.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
EC50: 1.3 nM (T. congolense), 18 nM (T. vivax)[1]
CRK12-IN-1 (compound 1) (10 mg/mL; 69 hours) is extremely potent against T.b. brucei and in animal models of T.b. brucei infection, as well as a potent inhibitor of T. congolensei (EC50 of 1.3 and 18 nM, respectively)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CRK12-IN-1 (5 mg/kg, s.c., twice 12 h apart for 4 days) can suppress parasitaemia below the level of detection in T. congolense infected calves, but parasitaemia quickly re-emerges following the cessation of treatment[1].
CRK12-IN-1 (10 mg free base/kg; s.c.; for 0.08-8 hours) has 74% of bioavailability with a half-life of about 1 hour in female NMRI mice[1].
CRK12-IN-1 (i.m. at 5 mg free base/kg or i.v. at 2.5 mg free base/kg; 0.25-120 hours) has a moderate clearance from the blood and a relatively short half-life (about1.8 h) in male ruminating Holstein-Friesian, and penetrate tissues beyond the vasculature[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1990479-14-5
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Molecular Weight 472.57
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Formula C20H26F2N4O3S2
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SMILES
O=S(N[C@@H]1CC[C@@H](NC2=NC(N)=C(C(C3=C(F)C=CC=C3F)=O)S2)CC1)(CC(C)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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