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SR-3029

Name: SR-3029
Brand: TargetMol
SKU: T3972
Price: 398 CNY
Availability: InStock
Rating: 5 (10 reviews)

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纯度: 99.64%

货号 T3972Cas号 1454585-06-8

别名 SR3029

SR-3029 具有 ATP 竞争性，有效抑制 CK1δ和 CK1ε，IC50值分别为 44 nM 和 260 nM，Ki 均为 97 nM。

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SR-3029

一键复制产品信息

很棒

纯度: 99.64%

货号 T3972 别名 SR3029Cas号 1454585-06-8

SR-3029 具有 ATP 竞争性，有效抑制 CK1δ和 CK1ε，IC50值分别为 44 nM 和 260 nM，Ki 均为 97 nM。

规格	价格	库存
1 mg	¥ 398	现货
5 mg	¥ 970	现货
10 mg	¥ 1,570	现货
25 mg	¥ 3,150	现货
50 mg	¥ 4,490	现货
1 mL x 10 mM (in DMSO)	¥ 1,050	现货

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产品介绍

SR-3029 AI Summary

SR-3029 exhibits oral bioavailability in C57BL6 mice with an F value of 13.0%, a half-life of 0.9 hours, an area under the curve (AUC) of 1153.08 ng∙hr/mL, a clearance rate of 49.0 mL/min/kg, and a maximum concentration (Cmax) of 1100.0 nM. It demonstrates significant inhibitory activity against CK1delta with an IC50 of 44.0 nM and CK1epsilon with an IC50 of 260.0 nM, and potent inhibition of CDK13 with an IC50 of 10.0 nM. The compound also displays antiproliferative activity against MDA-MB-231 cells with an EC50 of 26.0 nM and affects cell viability in a cell-type dependent manner, decreasing growth in HEK293T cells but potentially increasing growth in U2OS cells. SR-3029 shows varying aqueous solubility, measured at 100.0 nM at pH 7.4, and affects the thermal stability of protein domains in a domain-specific manner, with Delta TM values ranging from significant increases to slight decreases. It inhibits CYP enzymes in human liver microsomes with a broad range of inhibition percentages (12.0% to 62.0%), except for CYP2D6, which it slightly activates (-3.0%). Moreover, SR-3029 exhibits apparent permeability in PAMPA assays with a Papp value of 0.4 × 10^-6 cm/s, and demonstrates varying half-lives in human, mouse, and rat liver microsomes, indicating its potential for further exploration in the development of CDK-targeted therapies..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	SR-3029 is a potent and highly specific CK1δ/CK1ε inhibitor.
靶点活性	FLT3:3000 nM, CDK6-CyclinD1:428 nM, Cdk4-CyclinD1:576 nM, CK1ε:260 nM, CDK6-CyclinD3:427 nM, CK1δ:44 nM, CDK4-CyclinD3:368 nM
别名	SR3029

化学信息

分子量	480.45
分子式	C₂₃H₁₉F₃N₈O
CAS No.	1454585-06-8
Smiles	Fc1cccc(c1)-n1cnc2c(NCc3nc4ccc(F)c(F)c4[nH]3)nc(nc12)N1CCOCC1
密度	1.62 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 45 mg/mL (93.66 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.16 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0814 mL	10.4069 mL	20.8138 mL	104.0691 mL
5 mM	0.4163 mL	2.0814 mL	4.1628 mL	20.8138 mL
10 mM	0.2081 mL	1.0407 mL	2.0814 mL	10.4069 mL
20 mM	0.1041 mL	0.5203 mL	1.0407 mL	5.2035 mL
50 mM	0.0416 mL	0.2081 mL	0.4163 mL	2.0814 mL