2. Cell Cycle/DNA Damage
  3. CDK
  4. Ulecaciclib

Ulecaciclib 是一种具有口服活性的细胞周期蛋白依赖激酶 (CDK) 抑制剂，对 CDKs 的 k i 为 0.62 μM (CDK2/Cyclin A)、0.2 nM (CDK4/Cyclin D1)、3 nM (CDK6/Cyclin D3) 和 0.63 μM (CDK7/Cyclin H)。Ulecaciclib 能够通过血脑屏障，具有良好的药代动力学特性。

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Ulecaciclib Chemical Structure

Ulecaciclib Chemical Structure

CAS No. : 2075750-05-7

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Ulecaciclib 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1][2][3].

IC50 & Target

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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MDA-MB-453 GI50
0.622 μM
Compound: 116
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
[PMID: 28156111]
MV4-11 GI50
0.01 μM
Compound: 116
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
[PMID: 28156111]
体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Ulecaciclib 相关抗体:

Cell Viability Assay[2]

Cell Line: U87, U251, T98G (mycoplasma-free); and MB453, Colo205, H460, A2780, PANC1, LNC, M229
Concentration: 0-10 μM
Incubation Time: 72 hours
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).
体内研究
(In Vivo)

Ulecaciclib (compound 2) (2 mg/kg for i.v.; 10 mg/kg for p.o.) demonstrates a significantly propensity to cross the blood brain barrier in mice, with the brain/plasma ratios are >1.2 (i.v.) or >0.7 (p.o.), respectively[2].
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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CDl nu/nu female mice (5-6 weeks old; injected with U87 GBM cells, s.c.)[2]
Dosage: 200 mg/kg
Administration: Oral gavage; daily; 21 days
Result: Reduced tumour growth markedly without any overt toxicity.
Animal Model: GBM orthotopic mouse xenograft models[2]
Dosage: 120 mg/kg
Administration: Oral gavage; daily for 2 days
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.
分子量

496.65

Formula

C25H33FN8S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Ulecaciclib 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ulecaciclib2075750-05-7CDKCyclin dependent kinaseantineoplasticcyclin-dependent kinaseblood brain barrieranti-tumorCNScentral nervous systemGBMU87U251T98Gmycoplasma-freeMB453Colo205H460A2780PANC1LNCM229Inhibitorinhibitorinhibit

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