标签归档：abemaciclib

Abemaciclib(Synonyms: LY2835219)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib (Synonyms: LY2835219) 纯度: 99.83%

Abemaciclib (LY2835219) 是具有选择性的 CDK4/6 抑制剂，能够抑制 CDK4/CDK6 的活性，IC50 分别为 2 nM 和 10 nM。

Abemaciclib(Synonyms: LY2835219)

Abemaciclib Chemical Structure

CAS No. : 1231929-97-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥600 In-stock
10 mg ￥900 In-stock
50 mg ￥1200 In-stock
100 mg ￥1500 In-stock
200 mg ￥1900 In-stock
500 mg ￥3500 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Abemaciclib 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • CNS-Penetrant Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Breast Cancer Compound Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Therapy Drug Library
  • Rare Diseases Drug Library

生物活性

Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

IC50 & Target[3]

Cdk4/cyclin D1

2 nM (IC50)

CDK6/cyclinD1

10 nM (IC50)

CDK9/cyclinT1

57 nM (IC50)

CDK5/p35

287 nM (IC50)

Cdk5/p25

355 nM (IC50)

CDK2/cyclinE

504 nM (IC50)

CDK7/Mat1/cyclinH1

3910 nM (IC50)

CDK1/cyclinB1

1627 nM (IC50)

PIM1

50 nM (IC50)

PIM2

3400 nM (IC50)

HIPK2

31 nM (IC50)

DYRK2

61 nM (IC50)

CK2

117 nM (IC50)

GSK3b

192 nM (IC50)

JNK3

389 nM (IC50)

FLT3 (D835Y)

403 nM (IC50)

FLT3

3960 nM (IC50)

DRAK1

659 nM (IC50)

体外研究
(In Vitro)

Abemaciclib reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells[1]. Abemaciclib shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM; Abemaciclib inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC50 values of 395, 260, and 463 nM, respectively[2]. Abemaciclib inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Abemaciclib (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor[1]. Abemaciclib (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

506.59

Formula

C27H32F2N8
CAS 号

1231929-97-7
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 : 5 mg/mL (9.87 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9740 mL 9.8699 mL 19.7398 mL
5 mM 0.3948 mL 1.9740 mL 3.9480 mL
10 mM — — —

*

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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂： 0.5% HEC

    Solubility: 3.33 mg/mL (6.57 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.5 mg/mL (0.99 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.99 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.5 mg/mL (0.99 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.99 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 4.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 0.5 mg/mL (0.99 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.99 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget.?2016 Mar 22;7(12):14803-13.

    [2]. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63.

    [3]. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37.
Cell Assay
[1]

Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer’s instructions. The interaction between Abemaciclib and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of <1 is synergistic and a ci of>1 is antagonistic.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Six-week-old BALB/c female nude mice are injected subcutaneously with OSC-19 (1×106) cells. When tumor sizes reach approximately 100 mm3, mice are randomized by tumor size and subjected to each treatment. At least 5 mice per treatment group are included. Each group of mice is dosed via daily oral gavage with vehicle, Abemaciclib (45 mg/kg/d or 90 mg/kg/d), RAD001 (5 mg/kg/d), or a combination of both. The Abemaciclib is dissolved in 1% HEC in 20 mM phosphate buffer (pH2.0). Tumor size and body weight are measured twice weekly. Tumor volumes are calculated using the following formula: V=(L×W2)/2. Mice are gavaged a final time on day 14 and sacrificed the following day. The tumors are removed for Western blot and immunohistochemistry.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget.?2016 Mar 22;7(12):14803-13.

    [2]. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63.

    [3]. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Abemaciclib-d8(Synonyms: LY2835219-d8)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib-d8 (Synonyms: LY2835219-d8)

Abemaciclib-d8 (LY2835219-d8) 是 Abemaciclib 的氘代物。Abemaciclib (LY2835219) 是具有选择性的 CDK4/6 抑制剂，能够抑制 CDK4/CDK6 的活性，IC50 分别为 2 nM 和 10 nM。

Abemaciclib-d8(Synonyms: LY2835219-d8)

Abemaciclib-d8 Chemical Structure

CAS No. : 2088650-53-5

规格 价格 是否有货
1 mg ￥6800 询问价格 & 货期
5 mg ￥15000 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

Abemaciclib-d8 (LY2835219-d8) is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

514.64

Formula

C27H24D8F2N8
CAS 号

2088650-53-5
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.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget.?2016 Mar 22;7(12):14803-13.

    [3]. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63.

    [4]. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Abemaciclib methanesulfonate(Synonyms: LY2835219 methanesulfonate)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib methanesulfonate (Synonyms: LY2835219 methanesulfonate) 纯度: 99.92%

Abemaciclib methanesulfonate (LY2835219 methanesulfonate) 是选择性的 CDK4/6 抑制剂，抑制 CDK4/CDK6 的 IC50 分别为 2 nM 和 10 nM。

Abemaciclib methanesulfonate(Synonyms: LY2835219 methanesulfonate)

Abemaciclib methanesulfonate Chemical Structure

CAS No. : 1231930-82-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥800 In-stock
5 mg ￥600 In-stock
10 mg ￥900 In-stock
50 mg ￥1200 In-stock
100 mg ￥1500 In-stock
200 mg ￥1900 In-stock
500 mg ￥3500 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Abemaciclib methanesulfonate 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library
  • Rare Diseases Drug Library

生物活性

Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively[1][2][3].

IC50 & Target[3]

Cdk4/cyclin D1

2 nM (IC50)

CDK6/cyclinD1

10 nM (IC50)

CDK2/cyclinE

504 nM (IC50)

CDK9/cyclinT1

57 nM (IC50)

CDK1/cyclinB1

1627 nM (IC50)

CDK7/Mat1/cyclinH1

3910 nM (IC50)

Cdk5/p25

355 nM (IC50)

CDK5/p35

287 nM (IC50)

PIM1

50 nM (IC50)

PIM2

3400 nM (IC50)

HIPK2

31 nM (IC50)

DYRK2

61 nM (IC50)

CK2

117 nM (IC50)

GSK3b

192 nM (IC50)

JNK3

389 nM (IC50)

FLT3 (D835Y)

403 nM (IC50)

FLT3

3960 nM (IC50)

DRAK1

659 nM (IC50)

体外研究
(In Vitro)

Abemaciclib (LY2835219) reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells[1]. Abemaciclib (LY2835219) shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM; Abemaciclib inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC50 values of 395, 260, and 463 nM, respectively[2]. Abemaciclib (LY2835219) inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Abemaciclib (LY2835219) (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor[1]. Abemaciclib (LY2835219) (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

602.70

Formula

C28H36F2N8O3S
CAS 号

1231930-82-7
运输条件

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

H2O : 125 mg/mL (207.40 mM; Need ultrasonic)

DMSO : 33.33 mg/mL (55.30 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6592 mL 8.2960 mL 16.5920 mL
5 mM 0.3318 mL 1.6592 mL 3.3184 mL
10 mM 0.1659 mL 0.8296 mL 1.6592 mL

*

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 (sealed storage, away from moisture)。-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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂： PBS

    Solubility: 25 mg/mL (41.48 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 0.5% HEC

    Solubility: 12.5 mg/mL (20.74 mM); Clear solution; Need ultrasonic

  • 3.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.15 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.15 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 4.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.15 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.15 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 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 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 5.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.15 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.15 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 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。

  • 6.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: 2 mg/mL (3.32 mM); Suspended solution; Need ultrasonic

  • 7.

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2 mg/mL (3.32 mM); Clear solution

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget. 2016 Mar 22;7(12):14803-13.

    [2]. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63.

    [3]. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37.

    [4]. Wu T, et al. Effect of abemaciclib (LY2835219) on enhancement of chemotherapeutic agents in ABCB1 and ABCG2 overexpressing cells in vitro and in vivo. Biochem Pharmacol. 2017 Jan 15;124:29-42.
Cell Assay
[1]

Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer’s instructions. The interaction between Abemaciclib (LY2835219) and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of < 1 is synergistic and a CI of > 1 is antagonistic.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Six-week-old BALB/c female nude mice are injected subcutaneously with OSC-19 (1×106) cells. When tumor sizes reach approximately 100 mm3, mice are randomized by tumor size and subjected to each treatment. At least 5 mice per treatment group are included. Each group of mice is dosed via daily oral gavage with vehicle, Abemaciclib (LY2835219) (45 mg/kg/d or 90 mg/kg/d), RAD001 (5 mg/kg/d), or a combination of both. The Abemaciclib (LY2835219) is dissolved in 1% HEC in 20 mM phosphate buffer (pH2.0). Tumor size and body weight are measured twice weekly. Tumor volumes are calculated using the following formula: V=(L × W2)/2 (L, Length; W, width). Mice are gavaged a final time on day 14 and sacrificed the following day. The tumors are removed for Western blot and immunohistochemistry.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget. 2016 Mar 22;7(12):14803-13.

    [2]. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63.

    [3]. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37.

    [4]. Wu T, et al. Effect of abemaciclib (LY2835219) on enhancement of chemotherapeutic agents in ABCB1 and ABCG2 overexpressing cells in vitro and in vivo. Biochem Pharmacol. 2017 Jan 15;124:29-42.

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Abemaciclib metabolite M2(Synonyms: LSN2839567)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib metabolite M2 (Synonyms: LSN2839567) 纯度: 99.82%

Abemaciclib metabolite M2 (LSN2839567) 是 Abemaciclib 的代谢物，为有效的 CDK4 和 CDK6 抑制剂，IC50 值为 1-3 nM。具有抗肿瘤活性。

Abemaciclib metabolite M2(Synonyms: LSN2839567)

Abemaciclib metabolite M2 Chemical Structure

CAS No. : 1231930-57-6

规格 价格 是否有货 数量
1 mg ￥3200 In-stock
5 mg ￥9600 In-stock
10 mg ￥16000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Abemaciclib metabolite M2 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity[1].

IC50 & Target[1]

CDK4

1-3 nM (IC50)

CDK6

1-3 nM (IC50)

分子量

478.54

Formula

C25H28F2N8
CAS 号

1231930-57-6
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
In Vitro: 

DMSO : 2 mg/mL (4.18 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0897 mL 10.4484 mL 20.8969 mL
5 mM — — —
10 mM — — —

*

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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.22 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.22 mM，饱和度未知) 的澄清溶液。

    以 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 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Teresa Burke, et al. Abstract 2830: The major human metabolites of abemaciclib are inhibitors of CDK4 and CDK6. Cancer Research. July 2016, 76 (14).

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Abemaciclib metabolite M20(Synonyms: LSN3106726)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib metabolite M20 (Synonyms: LSN3106726) 纯度: 98.24%

Abemaciclib metabolite M20 (LSN3106726) 是 Abemaciclib 的活性代谢物，是一种选择性 CDK4/6 抑制剂，可用于癌症的相关研究。

Abemaciclib metabolite M20(Synonyms: LSN3106726)

Abemaciclib metabolite M20 Chemical Structure

CAS No. : 2138499-06-4

规格 价格 是否有货 数量
1 mg ￥1800 In-stock
5 mg ￥3500 In-stock
10 mg ￥5500 In-stock
25 mg ￥9900 In-stock
50 mg ￥16500 In-stock
100 mg ￥22500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Abemaciclib metabolite M20 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor for the treatment of cancer[1].

IC50 & Target[1]

CDK4

 

CDK6

 

分子量

522.59

Formula

C27H32F2N8O
CAS 号

2138499-06-4
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
In Vitro: 

DMSO : 5 mg/mL (9.57 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9135 mL 9.5677 mL 19.1355 mL
5 mM 0.3827 mL 1.9135 mL 3.8271 mL
10 mM — — —

*

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。
参考文献

  • [1]. Richard Paul Beckmann, et al. Combination therapy with notch and cdk4/6 inhibitors for the treatment of cancer. WO2017180389A1.

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Abemaciclib metabolite M18 hydrochloride(Synonyms: LSN3106729 hydrochloride)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib metabolite M18 hydrochloride (Synonyms: LSN3106729 hydrochloride) 纯度: 99.01%

Abemaciclib metabolite M18 (LSN3106729) hydrochloride，Abemaciclib 的代谢物，是一种具有抗肿瘤活性的 CDK 抑制剂。Abemaciclib metabolite M18 hydrochloride 和 CRBN 配体可用于设计 PROTAC CDK4/6 降解剂。

Abemaciclib metabolite M18 hydrochloride(Synonyms: LSN3106729 hydrochloride)

Abemaciclib metabolite M18 hydrochloride Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4090 In-stock
5 mg ￥3500 In-stock
10 mg ￥5500 In-stock
25 mg ￥9900 In-stock
50 mg ￥16500 In-stock
100 mg ￥22500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Abemaciclib metabolite M18 hydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

Abemaciclib metabolite M18 (LSN3106729) hydrochloride, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1].

IC50 & Target[1]

CDK4

 

CDK6

 

分子量

531.00

Formula

C25H29ClF2N8O
运输条件

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (235.40 mM; Need ultrasonic)

H2O : 100 mg/mL (188.32 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8832 mL 9.4162 mL 18.8324 mL
5 mM 0.3766 mL 1.8832 mL 3.7665 mL
10 mM 0.1883 mL 0.9416 mL 1.8832 mL

*

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 (sealed storage, away from moisture)。-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。
参考文献

  • [1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non–Small Cell Lung Cancer: A Phase Ib Study.

    [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.

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Abemaciclib-d7(Synonyms: LY2835219-d7)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib-d7 (Synonyms: LY2835219-d7)

Abemaciclib-d7 (LY2835219-d7) 是 Abemaciclib 的氘代物。Abemaciclib (LY2835219) 是具有选择性的 CDK4/6 抑制剂，能够抑制 CDK4/CDK6 的活性，IC50 分别为 2 nM 和 10 nM。

Abemaciclib-d7(Synonyms: LY2835219-d7)

Abemaciclib-d7 Chemical Structure

CAS No. : 2225881-57-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Abemaciclib-d7 (LY2835219-d7) is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

513.64

Formula

C27H25D7F2N8
CAS 号

2225881-57-0
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.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget.?2016 Mar 22;7(12):14803-13.

    [3]. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63.

    [4]. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37.

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Abemaciclib metabolite M18(Synonyms: LSN3106729)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib metabolite M18 (Synonyms: LSN3106729)

Abemaciclib metabolite M18 (LSN3106729)，Abemaciclib 的代谢物， 是一种具有抗肿瘤活性的 CDK 抑制剂。Abemaciclib metabolite M18 和 CRBN 配体可用于设计 PROTAC CDK4/6 降解剂。

Abemaciclib metabolite M18(Synonyms: LSN3106729)

Abemaciclib metabolite M18 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Abemaciclib metabolite M18 的其他形式现货产品:

Abemaciclib metabolite M18 hydrochloride

生物活性

Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1].

IC50 & Target[1]

CDK4

 

CDK6

 

分子量

494.54

Formula

C25H28F2N8O
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.
参考文献

  • [1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non–Small Cell Lung Cancer: A Phase Ib Study.

    [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Abemaciclib metabolite M20-d8(Synonyms: LSN3106726-d8)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib metabolite M20-d8 (Synonyms: LSN3106726-d8)

Abemaciclib metabolite M20-d8 (LSN3106726-d8) 是 Abemaciclib metabolite M20 的氘代物。Abemaciclib metabolite M20 (LSN3106726) 是 Abemaciclib 的活性代谢物，是一种选择性 CDK4/6 抑制剂。

Abemaciclib metabolite M20-d8(Synonyms: LSN3106726-d8)

Abemaciclib metabolite M20-d8 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Abemaciclib metabolite M20-d8 (LSN3106726-d8) is the deuterium labeled Abemaciclib metabolite M20. Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor[1].

IC50 & Target[1]

CDK4

 

CDK6

 

分子量

530.64

Formula

C27H24D8F2N8O
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.
参考文献

  • [1]. Morschhauser F, et al. Clinical activity of abemaciclib in patients with relapsed or refractory mantle cell lymphoma – a phase II study. Haematologica. 2021;106(3):859-862. Published 2021 Mar 1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Abemaciclib metabolite M20-d8(Synonyms: LSN3106726-d8)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib metabolite M20-d8 (Synonyms: LSN3106726-d8)

Abemaciclib metabolite M20-d8 (LSN3106726-d8) 是 Abemaciclib metabolite M20 的氘代物。Abemaciclib metabolite M20 (LSN3106726) 是 Abemaciclib 的活性代谢物，是一种选择性 CDK4/6 抑制剂。

Abemaciclib metabolite M20-d8(Synonyms: LSN3106726-d8)

Abemaciclib metabolite M20-d8 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Abemaciclib metabolite M20-d8 (LSN3106726-d8) is the deuterium labeled Abemaciclib metabolite M20. Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor[1].

IC50 & Target[1]

CDK4

 

CDK6

 

分子量

530.64

Formula

C27H24D8F2N8O
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.
参考文献

  • [1]. Morschhauser F, et al. Clinical activity of abemaciclib in patients with relapsed or refractory mantle cell lymphoma – a phase II study. Haematologica. 2021;106(3):859-862. Published 2021 Mar 1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Abemaciclib metabolite M20-d8(Synonyms: LSN3106726-d8)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib metabolite M20-d8 (Synonyms: LSN3106726-d8)

Abemaciclib metabolite M20-d8 (LSN3106726-d8) 是 Abemaciclib metabolite M20 的氘代物。Abemaciclib metabolite M20 (LSN3106726) 是 Abemaciclib 的活性代谢物，是一种选择性 CDK4/6 抑制剂。

Abemaciclib metabolite M20-d8(Synonyms: LSN3106726-d8)

Abemaciclib metabolite M20-d8 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Abemaciclib metabolite M20-d8 (LSN3106726-d8) is the deuterium labeled Abemaciclib metabolite M20. Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor[1].

IC50 & Target[1]

CDK4

 

CDK6

 

分子量

530.64

Formula

C27H24D8F2N8O
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.
参考文献

  • [1]. Morschhauser F, et al. Clinical activity of abemaciclib in patients with relapsed or refractory mantle cell lymphoma – a phase II study. Haematologica. 2021;106(3):859-862. Published 2021 Mar 1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Abemaciclib metabolite M18-d8(Synonyms: LSN3106729-d8)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib metabolite M18-d8 (Synonyms: LSN3106729-d8)

Abemaciclib metabolite M18-d8 (LSN3106729-d8) 是 Abemaciclib metabolite M18 的氘代物。Abemaciclib metabolite M18 (LSN3106729)，Abemaciclib 的代谢物， 是一种具有抗肿瘤活性的 CDK 抑制剂。Abemaciclib metabolite M18 和 CRBN 配体可用于设计 PROTAC CDK4/6 降解剂。

Abemaciclib metabolite M18-d8(Synonyms: LSN3106729-d8)

Abemaciclib metabolite M18-d8 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Abemaciclib metabolite M18-d8 (LSN3106729-d8) is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

502.59

Formula

C25H20D8F2N8O
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.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.

    [3]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non–Small Cell Lung Cancer: A Phase Ib Study.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Abemaciclib metabolite M18-d8(Synonyms: LSN3106729-d8)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib metabolite M18-d8 (Synonyms: LSN3106729-d8)

Abemaciclib metabolite M18-d8 (LSN3106729-d8) 是 Abemaciclib metabolite M18 的氘代物。Abemaciclib metabolite M18 (LSN3106729)，Abemaciclib 的代谢物， 是一种具有抗肿瘤活性的 CDK 抑制剂。Abemaciclib metabolite M18 和 CRBN 配体可用于设计 PROTAC CDK4/6 降解剂。

Abemaciclib metabolite M18-d8(Synonyms: LSN3106729-d8)

Abemaciclib metabolite M18-d8 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Abemaciclib metabolite M18-d8 (LSN3106729-d8) is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

502.59

Formula

C25H20D8F2N8O
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.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.

    [3]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non–Small Cell Lung Cancer: A Phase Ib Study.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Abemaciclib metabolite M18-d8(Synonyms: LSN3106729-d8)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib metabolite M18-d8 (Synonyms: LSN3106729-d8)

Abemaciclib metabolite M18-d8 (LSN3106729-d8) 是 Abemaciclib metabolite M18 的氘代物。Abemaciclib metabolite M18 (LSN3106729)，Abemaciclib 的代谢物， 是一种具有抗肿瘤活性的 CDK 抑制剂。Abemaciclib metabolite M18 和 CRBN 配体可用于设计 PROTAC CDK4/6 降解剂。

Abemaciclib metabolite M18-d8(Synonyms: LSN3106729-d8)

Abemaciclib metabolite M18-d8 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Abemaciclib metabolite M18-d8 (LSN3106729-d8) is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

502.59

Formula

C25H20D8F2N8O
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.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.

    [3]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non–Small Cell Lung Cancer: A Phase Ib Study.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Abemaciclib metabolite M2-d6(Synonyms: LSN2839567-d6)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib metabolite M2-d6 (Synonyms: LSN2839567-d6)

Abemaciclib metabolite M2-d6 (LSN2839567-d6) 是 Abemaciclib metabolite M2 的氘代物。Abemaciclib metabolite M2 (LSN2839567) 是 Abemaciclib 的代谢物，为有效的 CDK4 和 CDK6 抑制剂，IC50 值为 1-3 nM。具有抗肿瘤活性。

Abemaciclib metabolite M2-d6(Synonyms: LSN2839567-d6)

Abemaciclib metabolite M2-d6 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Abemaciclib metabolite M2-d6 (LSN2839567-d6) is the deuterium labeled Abemaciclib metabolite M2. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

484.58

Formula

C25H22D6F2N8
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.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Teresa Burke, et al. Abstract 2830: The major human metabolites of abemaciclib are inhibitors of CDK4 and CDK6. Cancer Research. July 2016, 76 (14).

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Abemaciclib metabolite M2-d6(Synonyms: LSN2839567-d6)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib metabolite M2-d6 (Synonyms: LSN2839567-d6)

Abemaciclib metabolite M2-d6 (LSN2839567-d6) 是 Abemaciclib metabolite M2 的氘代物。Abemaciclib metabolite M2 (LSN2839567) 是 Abemaciclib 的代谢物，为有效的 CDK4 和 CDK6 抑制剂，IC50 值为 1-3 nM。具有抗肿瘤活性。

Abemaciclib metabolite M2-d6(Synonyms: LSN2839567-d6)

Abemaciclib metabolite M2-d6 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Abemaciclib metabolite M2-d6 (LSN2839567-d6) is the deuterium labeled Abemaciclib metabolite M2. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

484.58

Formula

C25H22D6F2N8
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.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Teresa Burke, et al. Abstract 2830: The major human metabolites of abemaciclib are inhibitors of CDK4 and CDK6. Cancer Research. July 2016, 76 (14).

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Abemaciclib metabolite M2-d6(Synonyms: LSN2839567-d6)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Abemaciclib metabolite M2-d6 (Synonyms: LSN2839567-d6)

Abemaciclib metabolite M2-d6 (LSN2839567-d6) 是 Abemaciclib metabolite M2 的氘代物。Abemaciclib metabolite M2 (LSN2839567) 是 Abemaciclib 的代谢物，为有效的 CDK4 和 CDK6 抑制剂，IC50 值为 1-3 nM。具有抗肿瘤活性。

Abemaciclib metabolite M2-d6(Synonyms: LSN2839567-d6)

Abemaciclib metabolite M2-d6 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Abemaciclib metabolite M2-d6 (LSN2839567-d6) is the deuterium labeled Abemaciclib metabolite M2. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

484.58

Formula

C25H22D6F2N8
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.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Teresa Burke, et al. Abstract 2830: The major human metabolites of abemaciclib are inhibitors of CDK4 and CDK6. Cancer Research. July 2016, 76 (14).

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务