1. Cell Cycle/DNA Damage Apoptosis
  2. CDK Apoptosis
  3. CA224

CA224 (Compound 1) 是一种选择性的、具有口服活性的 Cdk4–cyclin D1 抑制剂, IC50 值为 6.2 µM。CA224 诱导细胞凋亡 (apoptosis),具有抗肿瘤活性。

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CA224 Chemical Structure

CA224 Chemical Structure

CAS No. : 883561-04-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC50 of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity[1].

IC50 & Target

cdk4-cyclin D1

6.2 μM (IC50)

cdk2-cyclin A

521 μM (IC50)

体外研究
(In Vitro)

CA224 (Compound 1) (48 h) shows antiproliferation activity against human cancer cell lines[1].
CA224 (18-48 h) blocks the growth of cancer cells at G0/G1 and G2/M phase of the cell cycle, and selectively kills SV40 large T-antigen transformed normal mouse embryonic liver cells (BNL SV A.8)[1][2].
CA224 (0-4 µM, 30 min) inhibits tubulin polymerization and enhances the depolymerization of stabilized tubulin protein[1].
CA224 (0-72 h) induces cell apoptosis in cancer cells[1].
CA224 (10 μM) shows 50%, 14%, 51% and 19% inhibition of CYP3A4, CYP2D6, CYP2C9, and CYP2C19, respectively[1].

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

Cell Proliferation Assay[1]

Cell Line: LS174T, PC-3, MiaPaCa, A549, Calu-1, NCI-H460, NCI-H1299, NCI-H358, BNL CL2 and BNL SV A.8
Concentration:
Incubation Time: 48 h
Result: Showed antiproliferation activity with IC50 values of 3.5, 6.2, 4.0, 3.5, 11.5, 2.0, 2.5, 2.2, 2.6 and 3.8 uM against LS174T, PC-3, MiaPaCa, A549, Calu-1, NCI-H460, NCI-H1299, NCI-H358, BNL CL2 and BNL SV A.8, respectively.

Cell Cycle Analysis[1][2]

Cell Line: A549, NCI-H1299, NCI-H358, BNL CL2, BNL SV A.8 and Calu-1
Concentration: IC50 concentration (IC70 for Calu-1)
Incubation Time: 24 h for A549, NCI-H1299 and Calu-1, 18 h for NCI-H358, 48 h for BNL CL2 and BNL SV A.8
Result: Induced a profound block at G2/M in A549 and NCI-H1299 cells. Maintained nocodazole- and paclitaxel-induced G2/M block in NCI-H358 cells. Exhibited prominent G2/M arrest in BNL CL2 cells. 31% of cells were detected in sub-G1 phase (control: 0%) in BNL SV A.8 cells. Retained the G0/G1 block in serum-starved p53-null Calu-1 cells.

Western Blot Analysis[1]

Cell Line: A549 and LS174T
Concentration: IC50 concentration; 1, 2, 3 and 4 µM for tubulin polymerization
Incubation Time: 24 h; 30 min for tubulin polymerization in A549 cells
Result: Induced p53, p21, and p27. Downregulated cyclin B1 and Cdk1. Inhibited tubulin polymerization in a dose-dependent manner and resulted in accumulation of unassembled tubulin in the supernatant.

Apoptosis Analysis[1]

Cell Line: A549, NCI-H460, NCI-H358, and NCI-H1299
Concentration: IC50 and IC70 concentration
Incubation Time: 24, 48 and 72 h
Result: Induces apoptotic cell death in a dose- and time-dependent manner.
体内研究
(In Vivo)

CA224 (Compound 1) (100 mg/kg; i.p.; once a day for 9 days) shows significant tumor growth inhibition without obvious toxicity[1].

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

Animal Model: The severe combined immunodeficient (SCID) mouse, lacking both T and B immune cells. Male mice weighing 18−25 g, 6−8 weeks of age for subcutaneous injection of HCT-116, female mice weighing 15−24 g, 6−8 weeks of age for subcutaneous injection of NCI-H460[1]
Dosage: 100 mg/kg
Administration: Intraperitoneal injection, once a day for 9 consecutive days
Result: Showed significant tumor growth inhibition in both HCT-116 and NCI-H460 tumor models without significant bodyweight loss.
Animal Model: BALB/c mice[1]
Dosage: 10 mg/kg (oral administration) or 1.0 mg/kg (intravenous injection)
Administration: Oral or intravenous injection (Pharmacokinetics Analysis)
Result: Pharmacokinetics parameters determined for CA224 after IV and PO administration[1].
Parameter IV (1 mg/kg) Oral (10 mg/kg)
t1/2,β (h) 0.33 1.16
AUC0-t (ng·h/mL) 187 172
AUC0-∞ (ng·h/mL) 189 182
Cmax (ng/mL) 371 190
Vd (L/Kg) 2.52 nd
Vdss (L/Kg) 1.76 nd
CL (mL/min/kg) 88.3 nd
Bioavailability - 9.6%
Time points considered
for t1/2,β calculation
0.5-2 h 1-4 h
分子量

354.44

Formula

C24H22N2O

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (282.14 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 2.8214 mL 14.1068 mL 28.2135 mL
5 mM 0.5643 mL 2.8214 mL 5.6427 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。-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

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.05 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

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。-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 2.8214 mL 14.1068 mL 28.2135 mL 70.5338 mL
5 mM 0.5643 mL 2.8214 mL 5.6427 mL 14.1068 mL
10 mM 0.2821 mL 1.4107 mL 2.8214 mL 7.0534 mL
15 mM 0.1881 mL 0.9405 mL 1.8809 mL 4.7023 mL
20 mM 0.1411 mL 0.7053 mL 1.4107 mL 3.5267 mL
25 mM 0.1129 mL 0.5643 mL 1.1285 mL 2.8214 mL
30 mM 0.0940 mL 0.4702 mL 0.9405 mL 2.3511 mL
40 mM 0.0705 mL 0.3527 mL 0.7053 mL 1.7633 mL
50 mM 0.0564 mL 0.2821 mL 0.5643 mL 1.4107 mL
60 mM 0.0470 mL 0.2351 mL 0.4702 mL 1.1756 mL
80 mM 0.0353 mL 0.1763 mL 0.3527 mL 0.8817 mL
100 mM 0.0282 mL 0.1411 mL 0.2821 mL 0.7053 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:
CA224
目录号:
HY-111207
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