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Samuraciclib hydrochloride

Name: Samuraciclib hydrochloride
Brand: TargetMol
SKU: T10898
Price: 116 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T10898Cas No. 1805789-54-1

Alias ICEC0942 hydrochloride, CT7001 hydrochloride

Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.

Samuraciclib hydrochloride

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Purity: 99.8%

Catalog No. T10898Alias ICEC0942 hydrochloride, CT7001 hydrochlorideCas No. 1805789-54-1

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$116	In Stock	In Stock
2 mg	$158	Backorder	Backorder
5 mg	$247	In Stock	In Stock
10 mg	$373	In Stock	In Stock
25 mg	$662	In Stock	In Stock
50 mg	$942	In Stock	In Stock
100 mg	$1,280	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$272	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.8%

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.
Targets&IC50	CDK9-CyclinT1:1.2 μM, CDK1-CyclinA:1.8 μM, CDK4-CyclinD1:49 μM, CDK6-CyclinD1:34 μM, CDK5-p35 NCK:9.4 μM, CDK2-CyclinA:578 nM, CDK7-CyclinH:41 nM
In vitro	Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment can promote apoptosis. Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment can induce cell cycle arrest. Samuraciclib (ICEC0942; 0-10 μM; 0-24 hours; HCT116 cells) treatment inhibited the phosphorylation of PolII CTD in HCT116 colon cancer cells in a dose- and time-dependent manner. ICEC0942 also inhibits the phosphorylation of CDK1, CDK2 and retinoblastoma. Samuraciclib (ICEC0942) inhibits the growth of MCF7, T47D, MDA-MB-231, HS578T, MDA-MB-468, MCF10A and HMEC cells with GI50 values of 0.18 μM, 0.32 μM, 0.33 μM, 0.21 μM, 0.22 μM It is 0.67 μM and 1.25 μM.
In vivo	Samuraciclib (ICEC0942; 100 mg / kg; oral tube; daily; 14 consecutive days; female nu / nu-BALB / c athymic nude mice) treatment inhibited tumor growth by 60% on day 14 with a significant reduction in PolII Ser2 and Ser5 phosphorylation in PBMC and tumors. The combination of Samuraciclib (ICEC0942) and ICI 47699 treatment showed complete stagnation of estrogen receptor (ER) positive tumor xenografts.
Synonyms	ICEC0942 hydrochloride, CT7001 hydrochloride

Chemical Properties

Molecular Weight	430.97
Formula	C₂₂H₃₁ClN₆O
Cas No.	1805789-54-1
Smiles	Cl.CC(C)c1cnn2c(NCc3ccccc3)cc(NC[C@H]3CCNC[C@@H]3O)nc12
Relative Density.	no data available

Storage & Solubility Information

Storage

store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 55 mg/mL (127.62 mM), Sonication is recommended.

DMSO: 25 mg/mL (58.01 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.64 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO/H2O

	1mg	5mg	10mg	50mg
1 mM	2.3203 mL	11.6017 mL	23.2035 mL	116.0174 mL
5 mM	0.4641 mL	2.3203 mL	4.6407 mL	23.2035 mL
10 mM	0.2320 mL	1.1602 mL	2.3203 mL	11.6017 mL
20 mM	0.1160 mL	0.5801 mL	1.1602 mL	5.8009 mL
50 mM	0.0464 mL	0.2320 mL	0.4641 mL	2.3203 mL

H2O

	1mg	5mg	10mg	50mg
100 mM	0.0232 mL	0.1160 mL	0.2320 mL	1.1602 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc