Home Cart Sign in  
Chemical Structure| 784210-88-4 Chemical Structure| 784210-88-4

Structure of RGB-286638 free base
CAS No.: 784210-88-4

Chemical Structure| 784210-88-4

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

RGB-286638 is an effective CDK inhibitor that inhibits cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 activities with IC50 values of 1, 2, 3, 4, 5, and 5 nM, respectively. It also inhibits GSK-3β, TAK1, Jak2, and MEK1 with IC50 values of 3, 5, 50, and 54 nM, respectively.

Synonyms: RGB-286638

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of RGB-286638 free base

CAS No. :784210-88-4
Formula : C29H35N7O4
M.W : 545.63
SMILES Code : O=C(NN1CCOCC1)NC2=CC=CC(C3=C4C(C5=CC=C(CN6CCN(CCOC)CC6)C=C5)=NN3)=C2C4=O
Synonyms :
RGB-286638
MDL No. :MFCD18633230

Safety of RGB-286638 free base

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of RGB-286638 free base

epigenetics
RTK
MAPK
PI3K-AKT
JAK-STAT
Hedgehog

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
RPMI8226 50 nM 24-48 hours RGB-286638 treatment resulted in MM cytotoxicity in vitro associated with inhibition of MM tumor growth and prolonged survival in vivo Leukemia. 2013 Dec;27(12):2366-75
OPM1 50 nM 24-48 hours RGB-286638 treatment resulted in MM cytotoxicity in vitro associated with inhibition of MM tumor growth and prolonged survival in vivo Leukemia. 2013 Dec;27(12):2366-75
U266 50 nM 24-48 hours RGB-286638 treatment resulted in MM cytotoxicity in vitro associated with inhibition of MM tumor growth and prolonged survival in vivo Leukemia. 2013 Dec;27(12):2366-75
H929 50 nM 24-48 hours RGB-286638 treatment resulted in MM cytotoxicity in vitro associated with inhibition of MM tumor growth and prolonged survival in vivo Leukemia. 2013 Dec;27(12):2366-75
MM.1R 50 nM 24-48 hours RGB-286638 treatment resulted in MM cytotoxicity in vitro associated with inhibition of MM tumor growth and prolonged survival in vivo Leukemia. 2013 Dec;27(12):2366-75
MM.1S 50 nM 24-48 hours RGB-286638 treatment resulted in MM cytotoxicity in vitro associated with inhibition of MM tumor growth and prolonged survival in vivo Leukemia. 2013 Dec;27(12):2366-75
SW13 1.25 nM, 2.5 nM 24-48 hours To evaluate the effect of RGB-286638 on SW13 cell proliferation, results showed that RGB-286638 in combination with OTS167 had a synergistic antiproliferative effect. J Exp Clin Cancer Res. 2022 Sep 23;41(1):282.
NCI-H295R 1.25 nM, 2.5 nM 48-72 hours To evaluate the effect of RGB-286638 on NCI-H295R cell proliferation, results showed that RGB-286638 in combination with OTS167 had a synergistic antiproliferative effect. J Exp Clin Cancer Res. 2022 Sep 23;41(1):282.
GSCs 0-20 µM 72 hours Evaluate the effect of RGB-286638 on the viability of GSCs, showing that about one-third of the tumor models exhibited high sensitivity to RGB-286638. Neurooncol Adv. 2020 Nov 5;2(1):vdaa151
GBM8 0-20 µM 72 hours Evaluate the effect of RGB-286638 on the viability of GBM8 primary cells, showing that low concentrations of RGB-286638 (IC50 0.01-0.03 µM) almost completely inhibited cell viability. Neurooncol Adv. 2020 Nov 5;2(1):vdaa151
U138 0-20 µM 72 hours Evaluate the effect of RGB-286638 on the viability of U138 cells, showing that low concentrations of RGB-286638 (IC50 0.01-0.03 µM) almost completely inhibited cell viability. Neurooncol Adv. 2020 Nov 5;2(1):vdaa151
T98G 0-20 µM 72 hours Evaluate the effect of RGB-286638 on the viability of T98G cells, showing that low concentrations of RGB-286638 (IC50 0.01-0.03 µM) almost completely inhibited cell viability. Neurooncol Adv. 2020 Nov 5;2(1):vdaa151
U251 0-20 µM 72 hours Evaluate the effect of RGB-286638 on the viability of U251 cells, showing that low concentrations of RGB-286638 (IC50 0.01-0.03 µM) almost completely inhibited cell viability. Neurooncol Adv. 2020 Nov 5;2(1):vdaa151
U87 0-20 µM 72 hours Evaluate the effect of RGB-286638 on the viability of U87 cells, showing that low concentrations of RGB-286638 (IC50 0.01-0.03 µM) almost completely inhibited cell viability. Neurooncol Adv. 2020 Nov 5;2(1):vdaa151

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nuþ /Nuþ mice Human ACC xenograft model Intravenous injection 20 mg/kg Three times weekly (Monday, Wednesday, Friday) for two weeks, followed by continuous administration via ALZET pump for five weeks To evaluate the antitumor efficacy of RGB-286638 in combination with OTS167 in the ACC xenograft model, results showed that the combination treatment significantly reduced tumor burden. J Exp Clin Cancer Res. 2022 Sep 23;41(1):282.
CB-17 SCID mice MM.1S xenograft model Intravenous injection 30 mg/kg and 40 mg/kg 5 consecutive days RGB-286638 treatment significantly suppressed 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. Treatment was also associated with improved survival, evidenced by first death at day 24 in controls versus day 43 in both treated groups. Leukemia. 2013 Dec;27(12):2366-75
Female athymic nude mice Intracranial injection model of GBM8 primary cells Tail vein injection 40 mg/kg/day 5 consecutive days Evaluate the effect of RGB-286638 on intracranial tumor growth of GBM8, showing that RGB-286638 significantly reduced tumor growth signals but did not significantly improve median survival (47 days vs 53 days). Neurooncol Adv. 2020 Nov 5;2(1):vdaa151

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01168882 Hematological Malignancies PHASE1 WITHDRAWN 2025-07-15 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.16mL

1.83mL

0.92mL

18.33mL

3.67mL

1.83mL

References

 

Historical Records

Categories