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RGB-286638 free base
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RGB-286638 free base图片
CAS NO:784210-88-4
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
RGB-286638 是一种有效的CDK抑制剂,抑制cyclin T1-CDK9cyclin B1-CDK1cyclin E-CDK2cyclin D1-CDK4cyclin E-CDK3p35-CDK5活性,IC50分别为 1,2,3,4,5 和 5 nM;同时可抑制 GSK-3β,TAK1,Jak2 和 MEK1,IC50值分别为 3,5,50,和 54 nM。
生物活性

RGB-286638 is aCDKinhibitor that inhibits the kinase activity ofcyclin T1-CDK9,cyclin B1-CDK1,cyclin E-CDK2,cyclin D1-CDK4,cyclin E-CDK3, andp35-CDK5withIC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibitsGSK-3β, TAK1,Jak2andMEK1, withIC50s of 3, 5, 50, and 54 nM.

IC50& Target[1]

T1-CDK9

1 nM (IC50)

cyclin B1-CDK1

2 nM (IC50)

cyclin E-CDK2

3 nM (IC50)

cyclin D1-CDK4

4 nM (IC50)

cyclin E-CDK3

5 nM (IC50)

p35-CDK5

5 nM (IC50)

cyclin H-CDK7

44 nM (IC50)

cyclin D3-CDK6

55 nM (IC50)

GSK-3β

3 nM (IC50)

JAK2

50 nM (IC50)

MEK1

54 nM (IC50)

Fms

1 nM (IC50)

TAK1

5 nM (IC50)

JNK1a1

17 nM (IC50)

JNK1a2

40 nM (IC50)

C-src

25 nM (IC50)

AMPK

41 nM (IC50)

体外研究
(In Vitro)

RGB-286638 is an indenopyrazole-derived CDK inhibitor (CDKI) with Ki-nanomolar activity against transcriptional CDKs. RGB-286638 inhibits several tyrosine and serine/threonine non-CDK enzymes, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1. The dose- and time-dependent effect of treatment with RGB-286638 (12.5-100nM) is investigated on the growth of human p53-wt (MM.1S, MM.1R, and H929) and p53-mutant (U266, OPM1, and RPMI) MM cells by MTT assay, assessing viability at 24 and 48 hours. The half-maximally effective concentrations (EC50) range between 20 and 70 nM at 48 hours. Dose-dependent differences in growth among p53-wt and -mutant cells are observed after 50nM treatment, with p53-wt MM.1S, MM.1R and H929 being slightly more sensitive to RGB-286638 treatment at 48h[1].

体内研究
(In Vivo)

Dose-finding studies with RGB-286638 identify 40 mg/kg/day IV treatment as the maximum tolerated dose in SCID mice. Five days IV treatment with RGB-286638 significantly suppresses MM tumor growth, with maximum TGI (%) noted at day 14 following end of treatment at 85.06% and 86.34% in the 30 mg/kg and 40 mg/kg treated cohorts respectively. The log10 cell kill (LCK Td: 4.5 days) is 1.6 for both treated groups. RGB-286638 treatment is also associated with improved survival, evidenced by first death at day 24 in controls versus day 43 in both treated groups. No toxic deaths occurred during this study: maximum percentage of body weight (BW) loss is observed on day 5 (8.4%) at 30 mg/kg dosage schedule, and on day 15 (9.9%) after 40 mg/kg dosing, with weight recovery in the following two weeks[1].

Clinical Trial
分子量

545.63

性状

Solid

Formula

C29H35N7O4

CAS 号

784210-88-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 2.6 mg/mL(4.77 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8327 mL9.1637 mL18.3274 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。