製品番号: HY-130250

SR-4835

Name: SR-4835
Brand: MedChemExpress
SKU: HY-130250
Price: 150.00 USD
Availability: InStock
Rating: 5 (21 reviews)

21 Cited Publications

カスタマーレビュー

Based on 21 publication(s) in Google Scholar

SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC₅₀=99 nM, K_d=98 nM; CDK13: K_d=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度 : 99.47%
CAS 番号: 2387704-62-1
分子式: C₂₁H₂₀Cl₂N₁₀O
分子量:499.36

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

SR-4835 構造式

CAS 番号: 2387704-62-1

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

IC₅₀ & Target

^[1]

CDK12

99 nM (IC₅₀)

CDK12

98 nM (Kd)

CDK13

4.9 nM (Kd)

CDK アイソフォーム固有の製品をすべて表示 :

体外実験

SR-4835 (90 nM; 0.5-48 hours) suppresses ATM and RAD51 protein levels^[1].
? SR-4835 inhibits CDK12/CDK13 which triggers intronic polyadenylation site cleavage and suppresses the expression of core DNA damage response proteins^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Western Blot Analysis^[1]

View Protocol

Cell Line:

MDA-MB-231 cells
Concentration:

90 nM
Incubation Time:

0.5, 6, 24, 48 hours
Result:

Suppressed ATM and RAD51 protein levels.

化学情報

CAS 番号 2387704-62-1
性状 Solid
分子量 499.36
分子式 C₂₁H₂₀Cl₂N₁₀O
Color Off-white to light brown
SMILES

CN1N=CC(N2C3=NC(N4CCOCC4)=NC(NCC5=NC6=C(N5)C=C(Cl)C(Cl)=C6)=C3N=C2)=C1
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	1 year
	-20°C	6 months

Publications (21)

All Bio/Physico-chemical AssayCell Proliferation/Viability Assay

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Journal Impact Factor

Mol Cell

The MYCN oncoprotein is an RNA-binding accessory factor of the nuclear exosome targeting complex. [Abstract]

2024 Jun 6;84(11):2070-2086.e20. PMID: 38703770
J Exp Clin Cancer Res

MYC up-regulation confers vulnerability to dual inhibition of CDK12 and CDK13 in high-risk Group 3 medulloblastoma. [Abstract]

2023 Aug 21;42(1):214. PMID: 37599362
Sci Adv

Cyclin K condensates bridge CDK12 to phosphorylate and drive oncogenic YAP activation in hepatocellular carcinoma. [Abstract]

2026 Jul 3;12(27):eaec6492. PMID: 42397909
Cancer Lett

CDK inhibition results in pharmacologic BRCAness increasing sensitivity to olaparib in BRCA1-WT and olaparib resistant in Triple Negative Breast Cancer. [Abstract]

2024 May 1:589:216820. PMID: 38574883
Cell Rep

CDK12 inhibition reveals melanoma dependence on the RUNX1/CBFβ complex for genomic stability. [Abstract]

2025 Nov 25;44(11):116495. PMID: 41176765
Breast Cancer Res

Systematic screening identifies ABCG2 as critical factor underlying synergy of kinase inhibitors with transcriptional CDK inhibitors. [Abstract]

2023 May 5;25(1):51. PMID: 37147730

SR-4835 purchased from MedChemExpress. Usage Cited in: Breast Cancer Res. 2023 May 5;25(1):51. [Abstract]

Proliferative response upon treatment with dose range of lapatinib in combination with transcriptional CDK inhibitor SR4835 (0.01 and 0.0316 µM) in Hs578T.

SR-4835 purchased from MedChemExpress. Usage Cited in: Breast Cancer Res. 2023 May 5;25(1):51. [Abstract]

Proliferative responses of dose ranges of transcriptional CDK inhibitors THZ531, THZ1, CDKI-73, PHA-767491, SR4835 and flavopiridol, alone, or in combination with KO143 (1 µM) or lapatinib (1 µM).
EMBO Rep

DDB1 engagement defines the selectivity of S656 analogs for cyclin K degradation over CDK inhibition. [Abstract]

2025 Jun;26(11):2836-2854. PMID: 40295725

SR-4835 purchased from MedChemExpress. Usage Cited in: EMBO Rep. 2025 Jun;26(11):2836-2854. [Abstract]

Inhibitory profile of S656, CR8, SR4835, HQ461, NCT02, THZ531 and SNS-032 compounds across 40 primary AML specimens in dose response assays. IC₅₀ values were determined after 6 days of incubation and normalized to DMSO control.
Sci Rep

2026 Apr 1.
J Biol Chem

The reversible inhibitor SR-4835 binds Cdk12/Cyclin K in a non-canonical G-loop conformation. [Abstract]

2024 Jan;300(1):105501. PMID: 38016516

SR-4835 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2024 Jan;300(1):105501. [Abstract]

dose-response curves for the inhibition of Cdk12/CycK and Cdk13/CycK by SR-4835. Radioactive kinase activity assays were performed for a concentration series of SR-4835 in presence of 0.2 μM indicated kinase and 0.2 mM [³²P]-γ-ATP. Assays were started by addition of 100 μM pS7-CTD_[3] substrate and incubated for 60 min. Measurements were performed in triplicates.

SR-4835 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2024 Jan;300(1):105501. [Abstract]

SR-4835 was tested at 0, 0.1, 1, 10, and 100 μM concentration against various CMGC kinases.
Biochem Biophys Res Commun

Interaction of CDK12 with NXF1 is a new node for the linking mechanism between transcription and transportation of mRNA. [Abstract]

2024 Nov 26:735:150608. PMID: 39270556
Oncologie

2023 Aug 8.
bioRxiv

2026 Jul 21.
Res Sq

2026 Apr 16.
bioRxiv

2026 Feb 20.
Res Sq

2025 Dec 18.
bioRxiv

2025 Nov 20.
Research Square Preprint

2024 Jan 31.
bioRxiv

2023 Jul 17.
University of Gothenburg

2023 Jun 27.
bioRxiv

2023 May 31.
Universidade de Lisboa

2021 Dec 21.

溶剤 & 溶解度

体外:

DMSO : 25 mg/mL (50.06 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)

H₂O : < 0.1 mg/mL (insoluble)

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

2.0026 mL

10.0128 mL

20.0256 mL

5 mM

0.4005 mL

2.0026 mL

4.0051 mL

10 mM

0.2003 mL

1.0013 mL

2.0026 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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 40% PEG300 5% Tween-80 45% Saline

Solubility: 2 mg/mL (4.01 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.

Protocol 2

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

Solubility: ≥ 0.89 mg/mL (1.78 mM); Clear solution

This protocol yields a clear solution of ≥ 0.89 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 (8.9 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 20% HP-β-CD in Saline

Solubility: 5 mg/mL (10.01 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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

All Cell Biology Signal Pathway Related Animals and Diseases

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.

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%

データシート (277 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Quereda V, et al. Therapeutic Targeting of CDK12/CDK13 in Triple-Negative Breast Cancer. Cancer Cell. 2019 Oct 8. pii: S1535-6108(19)30424-6. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0026 mL	10.0128 mL	20.0256 mL	50.0641 mL
	5 mM	0.4005 mL	2.0026 mL	4.0051 mL	10.0128 mL
	10 mM	0.2003 mL	1.0013 mL	2.0026 mL	5.0064 mL
	15 mM	0.1335 mL	0.6675 mL	1.3350 mL	3.3376 mL
	20 mM	0.1001 mL	0.5006 mL	1.0013 mL	2.5032 mL
	25 mM	0.0801 mL	0.4005 mL	0.8010 mL	2.0026 mL
	30 mM	0.0668 mL	0.3338 mL	0.6675 mL	1.6688 mL
	40 mM	0.0501 mL	0.2503 mL	0.5006 mL	1.2516 mL
	50 mM	0.0401 mL	0.2003 mL	0.4005 mL	1.0013 mL

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SR-4835

21 Cited Publications

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SR-4835

MedChemExpress（MCE）の使用を引用している文献 SR-4835

CDK アイソフォーム固有の製品をすべて表示

生物活性