Ulecaciclib
Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics.
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- No. CAS: 2075750-05-7
- Fòrmula: C25H33FN8S
- Peso molecular:496.65
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Actividad biológica
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cdk2/cyclin A 0.62 μM (Ki) |
Cdk4/cyclin D1 0.2 nM (Ki) |
cdk6/cyclin D3 3 nM (Ki) |
cdk7-cyclin H 0.63 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| MDA-MB-453 | GI50 |
0.622 μM
Compound: 116
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Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay
Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay
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[PMID: 28156111] |
| MV4-11 | GI50 |
0.01 μM
Compound: 116
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Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay
Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay
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[PMID: 28156111] |
Ulecaciclib (compound 2) (40 min) displays inhibitory effect on CDK kinase with Ki values of 0.62 μM (CDK2/A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), 0.63 μM (CDK7/H), respectively[2].
Ulecaciclib (72 h) exhibits a strong antiproliferative activity against leukemia cells with a growth inhibition GI50 value of 10 nM[2].
Ulecaciclib (72 h) inhibits tumor growth with GI50s range from 0.04-5.09 μM and inhibits Ovarian A2780 with an GI50 value of 40 nM, in particularly[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87, U251, T98G (mycoplasma-free); and MB453, Colo205, H460, A2780, PANC1, LNC, M229
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Concentration:0-10 μM
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Incubation Time:72 hours
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Result:Inhibited cancer cells growth with GI50s of 2.17 μM (U87), 5.09 μM (U251), 4.18 μM (T98G), 0.62 μM (MB453), 1.55 μM (Colo205), 0.41 μM (H460), 0.04 μM (A2780), 1.21 μM (PANC1), 0.28 μM (LNC), 0.83 μM (M229).
Ulecaciclib (200 mg/kg; p.o.; daily; 21 d) displays in vivo anti-tumour efficacy in mice[2].
Ulecaciclib (25 mg/kg; p.o.; daily; 10 d) demonstrates significant anti-tumour efficacy at lower doses in combination with TMZ (5 mg/kg; p.o.; 5 d/week; 2 weeks) in mice[2].
Ulecaciclib (compound A) (50 mg/kg; p.o.) shows an oral bioavailability of about 21.8%, and good pharmacokinetic profile with Tmax of 6.67 h and an half- of 8.34 h, while Cmax =643 ng/mL, AUC(0-24) =9543 ng•h/mL in male cynomolgus monkeys[3].
Pharmacokinetic of Ulecaciclib in cynomolgus monkeys[3]
| Route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC(0-t) (h•ng/mL) | AUC(0-∞) (h•ng/mL) | Vd (L/kg) | CL (mL/min/kg) | MRT(0-t) (h) | F (%) |
| i.v. | 5 | 6.53 | / | 447 | 4187 | 4560 | 9.79 | 19.4 | 6.64 | / |
| p.o. | 50 | 8.34 | 6.67 | 643 | 9543 | 7305 | / | / | 10.4 | 21.8 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CDl nu/nu female mice (5-6 weeks old; injected with U87 GBM cells, s.c.)[2]
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Dosage:200 mg/kg
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Administration:Oral gavage; daily; 21 days
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Result:Reduced tumour growth markedly without any overt toxicity.
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Animal Model:GBM orthotopic mouse xenograft models[2]
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Dosage:120 mg/kg
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Administration:Oral gavage; daily for 2 days
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Result:Inhibited tumor growth on day 21 and increased life span ratio (ILS) of 154.8% for teated mice.
ILS = (DaysT - DaysC)/DaysC, where DaysC = days survived by control group and DaysT = days survived by treatment group.
Chemical Information
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No. CAS 2075750-05-7
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Peso molecular 496.65
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Fòrmula C25H33FN8S
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SMILES
FC1=C(C2=C(C)N=C(NC3CCCC3)S2)N=C(NC4=NC=C(CN5CCN(CC5)CC)C=C4)N=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ulecaciclib Related Classifications
HY-147409 Related Classifications
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