RGB-286638 (free base)

Product Name: RGB-286638 (free base)
CAS No.: 784210-88-4
Chemical Name: RGB-286638 (free base)
Synonyms: CS-2608;CS-2607;RGB-286638 (free base);RGB-286638;RGB 286638;RGB-286638;2,6-DIBROMO-9,10-DI(1-NAPHTHYL)ANTHRACENE;1-[3-[4-[[4-(2-methoxyethyl)piperazin-1-yl]methyl]phenyl]-4-oxo-1H-indeno[1,2-c]pyrazol-5-yl]-3-morpholin-4-ylurea;1-(3-(4-((4-(2-Methoxyethyl)piperazin-1-yl)methyl)phenyl)-4-oxo-1,4-dihydroindeno[1,2-c]pyrazol-5-yl)-3-morpholinourea;N-[1,4-Dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N'-4-morpholinylurea;Urea,N-(1,4-dihydro-3-(4-((4-(2-methoxyethyl)-1-piperazinyl)methyl)phenyl)-4-oxoindeno(1,2-c)pyrazol-5-yl)-n'-4-morpholinyl;Urea, N-[1,4-dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N'-4-morpholinyl-
CBNumber: CB52668715
Molecular Formula: C29H35N7O4
Formula Weight: 545.63
MOL File: 784210-88-4.mol

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RGB-286638 (free base) Property

Density: 1.39±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMF: 3 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:20): 0.05 mg/ml; Ethanol: Partially soluble
pka: 9.19±0.20(Predicted)
form: Powder
color: Light yellow to green yellow

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 29499
Product name: RGB-286638
Packaging: 100mg
Price: $86
Updated: 2024/03/01

Cayman Chemical

Product number: 29499
Product name: RGB-286638
Packaging: 500mg
Price: $336
Updated: 2024/03/01

Cayman Chemical

Product number: 29499
Product name: RGB-286638
Packaging: 250mg
Price: $189
Updated: 2024/03/01

AK Scientific

Product number: 6498CS
Product name: RGB-286638freebase
Packaging: 250mg
Price: $297
Updated: 2021/12/16

ChemScene

Product number: CS-3452
Product name: RGB-286638freebase
Purity: 98.07%
Packaging: 10mg
Price: $300
Updated: 2021/12/16

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RGB-286638 (free base) Chemical Properties,Usage,Production

Uses

RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.

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].

IC 50

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)

References

[1] Cirstea D, et al. Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia. 2013 Dec;27(12):2366-75. DOI:10.1038/leu.2013.194

RGB-286638 (free base) Preparation Products And Raw materials

Raw materials

Preparation Products

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RGB-286638 (free base) Suppliers

China 64 United States 9 Global 73

Shanghai Boyle Chemical Co., Ltd.

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MedChemexpress LLC

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Shanghai YuanYe Biotechnology Co., Ltd.

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Target molecule Corp.

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784210-88-4, RGB-286638 (free base)Related Search:

BAM15 (3aR,6aR)-N-(4-((3-ethynylphenyl)amino)-7-methoxyquinazolin-6-yl)-1-methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxamide TG4-155 PH 797804 NVP-TAE684 Hydroxylamine-O-sulfonic acid Carbon tetrabromide Cyclopropylboronic acid XL-647 N-[3-[4-[4-[(Cyclohexylmethylsulfonyl)amino]butyl]piperazin-1-yl]phenyl]acetamide

RGB-286638 (free base)

N-[1,4-Dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N'-4-morpholinylurea

2,6-DIBROMO-9,10-DI(1-NAPHTHYL)ANTHRACENE

CS-2607

CS-2608

RGB-286638;RGB 286638;RGB-286638

1-[3-[4-[[4-(2-methoxyethyl)piperazin-1-yl]methyl]phenyl]-4-oxo-1H-indeno[1,2-c]pyrazol-5-yl]-3-morpholin-4-ylurea

Urea, N-[1,4-dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N'-4-morpholinyl-

RGB-286638,inhibit,MAP2K,RGB286638 free base,Glycogen synthase kinase-3,MAPKK,RGB 286638,Glycogen synthase kinase 3,MEK,RGB 286638 free base,Mitogen-activated protein kinase kinase,RGB286638,JAK,GSK-3,Janus kinase,Cyclin dependent kinase,CDK,Inhibitor

Urea,N-(1,4-dihydro-3-(4-((4-(2-methoxyethyl)-1-piperazinyl)methyl)phenyl)-4-oxoindeno(1,2-c)pyrazol-5-yl)-n'-4-morpholinyl

1-(3-(4-((4-(2-Methoxyethyl)piperazin-1-yl)methyl)phenyl)-4-oxo-1,4-dihydroindeno[1,2-c]pyrazol-5-yl)-3-morpholinourea

784210-88-4

C29H35N7O4

Inhibitors