1. Cell Cycle/DNA Damage
  2. CDK
  3. BS-194

BS-194 是一种具有口服活性的、有效的 CDK 选择性抑制剂。BS-194 抑制 CDK2、CDK1、CDK5、CDK7 和 CDK9IC50 值分别为 3、30、30、250 和 90 nM。BS-194 有效地抑制癌细胞增殖。BS-194 可用于乳腺癌、结肠癌等癌症的研究。

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BS-194 Chemical Structure

BS-194 Chemical Structure

CAS No. : 1092443-55-4

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5 mg ¥2100
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10 mg ¥3200
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, CDK9 (IC50s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer[1].

IC50 & Target[1]

CDK2

3 nM (IC50)

CDK1

30 nM (IC50)

CDK5

30 nM (IC50)

CDK7

250 nM (IC50)

CDK9

90 nM (IC50)

体外研究
(In Vitro)

BS-194 (compound 4k, 72 h) inhibits various cancer cells (MCF-7, MDA-MB-231, MCF-10A, CPLO-205, HCT-116, A549, SaOS2, PC3 ,HepG2, SK-Ov-3) growth, with IC50 values ranging from 100 nM to 1 μM[1].
BS-194 (10 μM, 24 h) promotes cell cycle arrest in in S and G2/M phases in HCT116 cells[1].
BS-194 (10 μM, 24 h) inhibits phosphorylation of CDK substrates, and promotes cyclin loss in HCT116 cells[1].

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

Cell Cycle Analysis[1]

Cell Line: HCT116
Concentration: 0, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Showed a significant reduction in G1, and increased in S and G2/M phases.

Western Blot Analysis[1]

Cell Line: HCT116
Concentration: 0, 0.1, 10, 20 μM
Incubation Time: 0, 0.1, 10, 20 μM
Result: Inhibited the phosphorylation of the CDK2 substrate RB (retinoblastoma) at Ser-780, Ser-795, Ser-801, Ser-807/Ser-811, and Thr-821.
Inhibited levels of cyclin A, cyclin B, and cyclin D1.
Inhibited phosphorylation of Thr-170 of CDK2.
体内研究
(In Vivo)

BS-194 (compound 4K, intraperitoneal injection, 5 or 10 mg/kg, twice daily for 14 days) inhibits tumor growth with no apparent toxicity in MCF-7 tumor xenografts[1].
BS-194 (i.p., i.v., p.o., 10 mg/kg) is orally bioavailable, with elimination half-lives of 147 min (i.p.), 210 min (i.v.), and 178 min (p.o.) respectively[1].
BS-194 (oral gavage, 25 mg/mL) reduces rapid RB and PolII (RNA polymerase II) phosphorylation, but recovery within 24 h in nu/nu-BALB/c athymic nude mice[1].
BS-194 (oral gavage, 25 mg/kg, daily for 14 days) inhibits tumor growth in HCT116 tumor xenografts, with no significant loss in animal weights[1].

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

Animal Model: Nude mice bearing MCF-7 cell[1]
Dosage: 5 or 10 mg/kg, twice daily for 14 days.
Administration: Intraperitoneal injection
Result: Inhibited tumor growth in a dose-dependent manner (30% and 40% reduction at 5 and 10 mg/kg dose, respectively).
Animal Model: HCT116 tumor xenografts[1]
Dosage: 25 mg/kg, daily for 14 days.
Administration: Oral gavage
Result: Inhibited tumor growth by 50% reduction at 25 mg/kg.
Decreased levels of Rb phosphorylation at Ser807/811 and Thr821 (in resected tumors).
Animal Model: Mice (pharmacokinetic assay)[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection, intravenous injection, oral administration
Result: Pharmacokinetic profile of BS-194 (compound 4k).
administration route dose (mg/kg) bioavail-ability (%) Cmax (min) T1/2 (min)
i.p. 10 73 30 147
p.o. 10 88 15 178
administration route dose (mg/kg) T1/2 (min) Cl (mL/min/kg) Vz
i.v. 10 210 5 1391
分子量

385.46

Formula

C20H27N5O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (259.43 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5943 mL 12.9715 mL 25.9430 mL
5 mM 0.5189 mL 2.5943 mL 5.1886 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

BS-194 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5943 mL 12.9715 mL 25.9430 mL 64.8576 mL
5 mM 0.5189 mL 2.5943 mL 5.1886 mL 12.9715 mL
10 mM 0.2594 mL 1.2972 mL 2.5943 mL 6.4858 mL
15 mM 0.1730 mL 0.8648 mL 1.7295 mL 4.3238 mL
20 mM 0.1297 mL 0.6486 mL 1.2972 mL 3.2429 mL
25 mM 0.1038 mL 0.5189 mL 1.0377 mL 2.5943 mL
30 mM 0.0865 mL 0.4324 mL 0.8648 mL 2.1619 mL
40 mM 0.0649 mL 0.3243 mL 0.6486 mL 1.6214 mL
50 mM 0.0519 mL 0.2594 mL 0.5189 mL 1.2972 mL
60 mM 0.0432 mL 0.2162 mL 0.4324 mL 1.0810 mL
80 mM 0.0324 mL 0.1621 mL 0.3243 mL 0.8107 mL
100 mM 0.0259 mL 0.1297 mL 0.2594 mL 0.6486 mL
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.

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产品名称:
BS-194
目录号:
HY-14372
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