製品番号: HY-18958

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CCT245737

(別名: SRA737)

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

CCT245737 (SRA737) is an orally active and seletive Chk1 inhibitor, with an IC₅₀ of 1.3 nM.

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純度: 99.48%
CAS 番号: 1489389-18-5
分子式: C₁₆H₁₆F₃N₇O
分子量:379.34

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

CCT245737 構造式

CAS 番号: 1489389-18-5

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (4)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

CCT245737 (SRA737) is an orally active and seletive Chk1 inhibitor, with an IC₅₀ of 1.3 nM.

IC₅₀ & Target^[1]

Chk1

1.3 nM (IC₅₀)

Chk2

2440 nM (IC₅₀)

ERK8

130 nM (IC₅₀)

PKD1

298 nM (IC₅₀)

RSK2

361 nM (IC₅₀)

RSK1

362 nM (IC₅₀)

FLT3

582 nM (IC₅₀)

MARK3

698 nM (IC₅₀)

NUAK1

711 nM (IC₅₀)

CLK2

1370 nM (IC₅₀)

BRSK1

1660 nM (IC₅₀)

AMPK

2970 nM (IC₅₀)

PHK

3470 nM (IC₅₀)

CDK2/CyclA

3850 nM (IC₅₀)

CDK1/CyclB

9030 nM (IC₅₀)

Checkpoint Kinase (Chk) アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	>10000 nM Compound: CCT245737	Antiproliferative activity against human A2780 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay Antiproliferative activity against human A2780 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay	[PMID: 38547734]
A549	IC₅₀	>10000 nM Compound: CCT245737	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay	[PMID: 38547734]
Calu-6	GI₅₀	0.046 μM Compound: Chemical probe: CCT245737	Cytotoxicity against human Calu-6 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay Cytotoxicity against human Calu-6 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay	[PMID: 26295308]
Calu-6	GI₅₀	0.32 μM Compound: Chemical probe: CCT245737	Cytotoxicity against human Calu-6 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay Cytotoxicity against human Calu-6 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay	[PMID: 26295308]
Calu-6	GI₅₀	0.41 μM Compound: Chemical probe: CCT245737	Cytotoxicity against human Calu-6 cells assessed as growth inhibition measured after 96 hrs by SRB assay Cytotoxicity against human Calu-6 cells assessed as growth inhibition measured after 96 hrs by SRB assay	[PMID: 26295308]
HCT-116	IC₅₀	>10000 nM Compound: CCT245737	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay	[PMID: 38547734]
HEK293	GI₅₀	1.387 μM Compound: CCT245737	Antiproliferative activity against human HEK293 cells after 72 hrs by MTS assay Antiproliferative activity against human HEK293 cells after 72 hrs by MTS assay	[PMID: 29684894]
HL-60	IC₅₀	>10000 nM Compound: CCT245737	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay	[PMID: 38547734]
HT-29	GI₅₀	0.09 μM Compound: Chemical probe: CCT245737	Cytotoxicity against human HT-29 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay Cytotoxicity against human HT-29 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay	[PMID: 26295308]
HT-29	GI₅₀	0.39 μM Compound: Chemical probe: CCT245737	Cytotoxicity against human HT-29 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay Cytotoxicity against human HT-29 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay	[PMID: 26295308]
HT-29	GI₅₀	0.7 μM Compound: Chemical probe: CCT245737	Cytotoxicity against human HT-29 cells assessed as growth inhibition measured after 96 hrs by SRB assay Cytotoxicity against human HT-29 cells assessed as growth inhibition measured after 96 hrs by SRB assay	[PMID: 26295308]
HT-29	GI₅₀	9.223 μM Compound: CCT245737	Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay	[PMID: 29684894]
HT-29	IC₅₀	>10000 nM Compound: CCT245737	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay	[PMID: 38547734]
HT-29	IC₅₀	176.62 nM Compound: CCT245737	Synergistic antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs in presence of 50 nM gemcitabine by CCK-8 assay Synergistic antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs in presence of 50 nM gemcitabine by CCK-8 assay	[PMID: 38547734]
MDA-MB-468	IC₅₀	>10000 nM Compound: CCT245737	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay	[PMID: 38547734]
MIA PaCa-2	GI₅₀	0.066 μM Compound: Chemical probe: CCT245737	Cytotoxicity against human MIA PaCa-2 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay Cytotoxicity against human MIA PaCa-2 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay	[PMID: 26295308]
MIA PaCa-2	GI₅₀	0.43 μM Compound: Chemical probe: CCT245737	Cytotoxicity against human MIA PaCa-2 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay Cytotoxicity against human MIA PaCa-2 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay	[PMID: 26295308]
MIA PaCa-2	GI₅₀	1.3 μM Compound: Chemical probe: CCT245737	Cytotoxicity against human MIA PaCa-2 cells assessed as growth inhibition measured after 96 hrs by SRB assay Cytotoxicity against human MIA PaCa-2 cells assessed as growth inhibition measured after 96 hrs by SRB assay	[PMID: 26295308]
MV4-11	IC₅₀	244.6 nM Compound: CCI245737	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 37584545]
MV4-11	IC₅₀	211.13 nM Compound: CCT-245737	Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD/TKD mutant incubated for 72 hrs by absorbance based microplate reader Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD/TKD mutant incubated for 72 hrs by absorbance based microplate reader	[PMID: 38389894]
OVCAR-3	IC₅₀	>10000 nM Compound: CCT245737	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay	[PMID: 38547734]
SW-620	GI₅₀	0.33 μM Compound: Chemical probe: CCT245737	Cytotoxicity against human SW620 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay Cytotoxicity against human SW620 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay	[PMID: 26295308]
SW-620	GI₅₀	1.8 μM Compound: Chemical probe: CCT245737	Cytotoxicity against human SW620 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay Cytotoxicity against human SW620 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay	[PMID: 26295308]
SW-620	GI₅₀	5.4 μM Compound: Chemical probe: CCT245737	Cytotoxicity against human SW620 cells assessed as growth inhibition measured after 96 hrs by SRB assay Cytotoxicity against human SW620 cells assessed as growth inhibition measured after 96 hrs by SRB assay	[PMID: 26295308]

体外実験

CCT245737 (10 μM) shows >80% inhibition of a panel of 124 kinases, including ERK8, PKD1, RSK2 and RSK1 with IC₅₀s of 130, 298, 361 and 362 nM^[1]. CCT245737 abrogates an VP-16-induced G2 checkpoint in HT29, SW620, MiaPaCa-2, and Calu6 cell lines, with IC₅₀s ranging from 30 to 220 nM^[2].

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

体内実験

CCT245737 (150 mg/kg p.o.) inhibits tumor growth in combination with LY 188011 (100 mg/kg iv) in HT29 colon cancer xenografts. CCT245737 (300 mg/kg, p.o.) also inhibits the LY 188011 (60 mg/kg iv) induced pSer296 CHK1 autophosphorylation at 24 h in SW620 human colon cancer xenografts^[1]. CCT245737 (150 mg/kg, p.o) alone significantly inhibits tumor growth in an Eμ-Myc mouse model of human B-cell lymphocytic leukemia^[2].

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

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1489389-18-5
性状 Solid
分子量 379.34
分子式 C₁₆H₁₆F₃N₇O
Color White to yellow
SMILES

FC(F)(F)C(C=NC(NC1=CN=C(C#N)C=N1)=C2)=C2NC[C@H]3CNCCO3
別名

SRA737
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Adv Sci (Weinh)

Pancancer Fine-Mapping of Mutational Intolerance Identifies CHEK1 as an Immunosuppressive Driver in Lung Adenocarcinoma. [Abstract]

2026 May;13(25):e21265. PMID: 41722056
Nucleic Acids Res

BTG3-dependent VCP/p97 nuclear translocation is required for efficient repair of UV-induced DNA lesions. [Abstract]

2025 Jul 8;53(13):gkaf626. PMID: 40626560

CCT245737 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2025 Jul 8;53(13):gkaf626. [Abstract]

XPC K63-linked ubiquitylation was enhanced by CHK1 inhibition. 293T cells were pretreated with 5 μM CHK1 inhibitor CCT245737 (CHK1i) for 2 h before UV, and XPC K63-ubiquitin modification was analyzed.

CCT245737 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2025 Jul 8;53(13):gkaf626. [Abstract]

CHK1 inhibition recapitulated the effect of BTG3 KO in delaying VCP/p97 nuclear translocation. Confocal microscopic imaging of VCP/p97 was conducted with HaCaT cells pretreated or not with CHK1i for 2 h.
Patent

US20240174977A1.
University of London

2021 Sep.

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (131.81 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6362 mL

13.1808 mL

26.3616 mL

5 mM

0.5272 mL

2.6362 mL

5.2723 mL

10 mM

0.2636 mL

1.3181 mL

2.6362 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

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

Mass Mass

濃度濃度

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分子量分子量

希釈計算機

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (13.18 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
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g
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

Cell Assay^[2]

Cytotoxicity is determined as the drug concentration that gives 50% inhibition of tumor cell proliferation (GI₅₀) using a 96 h Sulforhodamine B (SRB) assay. Inhibition of intracellular CHK1 activity is measured using a cell based ELISA for the abrogation of an VP-16 induced G2 checkpoint (mitosis induction assay, MIA). The IC₅₀ for G2 checkpoint abrogation (MIA) is determined in the presence of nocodazole using UCN01 as a positive control. The activity index (AI) is used as a measure of the compounds ability to induce mitosis relative to its toxicity (i.e., ratio of MIA IC₅₀: 96 h SRB GI₅₀). Routine potentiation studies are carried out using a fixed concentration (GI₅₀) of either LY 188011 or SN38 in combination with a range of CCT245737 concentrations to determine the combination GI₅₀ of CCT245737. The ability of CCT245737 to enhance LY 188011 or SN38 cell killing is expressed as a potentiation index (PI) equal to the ratio of the GI₅₀ for CCT245737 alone versus the combination GI₅₀ for CCT245737. PI values > 1 indicate potentiation of the genotoxic activity. In addition, a series of experiments is carried out using fixed, non- or minimally toxic concentrations of CCT245737 (≤GI₂₀) with a range of different concentrations of LY 188011 or SN38 to determine the extent to which CCT245737 enhances drug cytotoxicity compared with the genotoxic agent alone, i.e. conventional PI (ratio GI₅₀ genotoxic alone: GI₅₀ genotoxic combined with non-toxic CCT245737 concentration, Con PI)^[2].

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

Animal Administration^[1]

Human HT29 colorectal carcinoma cells are injected s.c into the flanks of female NCr athymic mice 6-8 weeks of age. Dosing commenced 5 days after transplantation when tumors reach a mean diameter of 5.5 mm. LY 188011 (100 mg/kg i.v.) is dosed in saline on days 0, 7 and 14 and compounds 4 (CCT245737) and 41 (150 mg/kg p.o.) in 10% DMSO 20% PEG 400, 5% Tween 80, 65% water, 24 and 48 h after each dose of LY 188011. Tumors are measured and body weights recorded three times weekly. Animals are culled on an individual basis when tumors reach a predetermined humane endpoint (mean diameter <15 mm)^[1].

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
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HNMR (2659 KB)
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参考文献

[1]. Osborne JD, et al. Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737). J Med Chem. 2016 Jun 9;59(11):5221-37. [Content Brief]

[2]. Walton MI, et al. The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eμ-MYC driven B-cell lymphoma. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6362 mL	13.1808 mL	26.3616 mL	65.9039 mL
	5 mM	0.5272 mL	2.6362 mL	5.2723 mL	13.1808 mL
	10 mM	0.2636 mL	1.3181 mL	2.6362 mL	6.5904 mL
	15 mM	0.1757 mL	0.8787 mL	1.7574 mL	4.3936 mL
	20 mM	0.1318 mL	0.6590 mL	1.3181 mL	3.2952 mL
	25 mM	0.1054 mL	0.5272 mL	1.0545 mL	2.6362 mL
	30 mM	0.0879 mL	0.4394 mL	0.8787 mL	2.1968 mL
	40 mM	0.0659 mL	0.3295 mL	0.6590 mL	1.6476 mL
	50 mM	0.0527 mL	0.2636 mL	0.5272 mL	1.3181 mL
	60 mM	0.0439 mL	0.2197 mL	0.4394 mL	1.0984 mL
	80 mM	0.0330 mL	0.1648 mL	0.3295 mL	0.8238 mL
	100 mM	0.0264 mL	0.1318 mL	0.2636 mL	0.6590 mL

Keywords

CCT245737

4 Cited Publications

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CCT245737

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MedChemExpress（MCE）の使用を引用している文献 CCT245737

Checkpoint Kinase (Chk) アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (4)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

CCT245737

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

MedChemExpress（MCE）の使用を引用している文献 CCT245737

Checkpoint Kinase (Chk) アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (4)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

CCT245737 関連分類

HY-18958 関連分類