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RGB-286638

Product Name
RGB-286638
CAS No.
784210-87-3
Chemical Name
RGB-286638
Synonyms
CS-1713;RGB-286638;RGB-286638 Dihydrochloride;N-[1,4-Dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N'-4-morpholinylurea hydrochloride
CBNumber
CB62667740
Molecular Formula
C29H37Cl2N7O4
Formula Weight
618.55458
MOL File
784210-87-3.mol
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RGB-286638 Property

storage temp. 
Store at -20°C
solubility 
DMSO: ≥ 150 mg/mL (242.50 mM)
form 
Powder
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

American Custom Chemicals Corporation
Product number
API0017268
Product name
RGB-286638
Purity
95.00%
Packaging
5MG
Price
$497.62
Updated
2021/12/16
ChemScene
Product number
CS-3453
Product name
RGB-286638
Purity
98.72%
Packaging
50mg
Price
$1320
Updated
2021/12/16
ChemScene
Product number
CS-3453
Product name
RGB-286638
Purity
98.72%
Packaging
100mg
Price
$2400
Updated
2021/12/16
Crysdot
Product number
CD31000796
Product name
RGB-286638
Purity
98+%
Packaging
100mg
Price
$1400
Updated
2021/12/16
Crysdot
Product number
CD31000796
Product name
RGB-286638
Purity
98+%
Packaging
50mg
Price
$770
Updated
2021/12/16
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RGB-286638 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 Preparation Products And Raw materials

Raw materials

Preparation Products

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RGB-286638 Suppliers

CHINA 43 United States 3 Global 46
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4769
Advantage
55
SPIRO PHARMA
Tel
Fax
-
Email
eric_feng1954@126.com
Country
China
ProdList
9248
Advantage
55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
Advantage
58
Amadis Chemical Company Limited
Tel
571-89925085
Fax
0086-571-89925065
Email
sales@amadischem.com
Country
China
ProdList
131957
Advantage
58
Musechem
Tel
+1-800-259-7612
Fax
+1-800-259-7612
Email
info@musechem.com
Country
United States
ProdList
4660
Advantage
60
Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
Country
China
ProdList
9729
Advantage
58
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
Advantage
58
Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
Advantage
58

784210-87-3, RGB-286638Related Search:


  • N-[1,4-Dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N'-4-morpholinylurea hydrochloride
  • RGB-286638
  • CS-1713
  • RGB-286638 Dihydrochloride
  • 784210-87-3
  • C29H35N7O42HCl