CBP501

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 204860

CAS#: 565434-85-7

Description: CBP501 is a peptide with G2 checkpoint-abrogating activity. G2 checkpoint inhibitor CBP501 inhibits multiple serine/threonine kinases, including MAPKAP-K2, C-Tak1, and CHK1, that phosphorylate serine 216 of the dual-specific phosphatase Cdc25C (cell division checkpoint 25 C); disruption of Cdc25C activity results in the inhibition of Cdc25C dephosphorylation of the mitotic cyclin-dependent kinase complex Cdc2/cyclin B, preventing entry into the mitotic phase of the cell cycle.


Chemical Structure

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CBP501
CAS# 565434-85-7

Theoretical Analysis

MedKoo Cat#: 204860
Name: CBP501
CAS#: 565434-85-7
Chemical Formula: C86H122F5N29O17
Exact Mass: 1927.94936
Molecular Weight: 1929.065
Elemental Analysis: C, 53.55; H, 6.37; F, 4.92; N, 21.06; O, 14.10

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: CBP501. Amino acid sequence: DArginine 4benzoylDphenylalanylDserylDtryptophylDseryl23456pentafluoroDphenylalanyl3cyclohexylDalanylDarginylDarginylDarginylDglutaminylDarginyl

IUPAC/Chemical Name: (2R,5R,8R,11R,14R,17R,20R,23R,26R,29R,32R,35R)-29-((1H-indol-3-yl)methyl)-35-amino-8-(3-amino-3-oxopropyl)-36-(4-benzoylphenyl)-20-(cyclohexylmethyl)-2,5,11,14,17-pentakis(3-guanidinopropyl)-26,32-bis(hydroxymethyl)-4,7,10,13,16,19,22,25,28,31,34-undecaoxo-23-((perfluorophenyl)methyl)-3,6,9,12,15,18,21,24,27,30,33-undecaazahexatriacontan-1-oic acid

InChi Key: DEZJGRPRBZSAKI-KMGSDFBDSA-N

InChi Code: InChI=1S/C86H122F5N29O17/c87-64-49(65(88)67(90)68(91)66(64)89)39-60(118-80(135)62(42-122)120-77(132)59(38-47-40-109-51-19-8-7-18-48(47)51)117-79(134)61(41-121)119-70(125)50(92)36-44-25-27-46(28-26-44)69(124)45-16-5-2-6-17-45)78(133)116-58(37-43-14-3-1-4-15-43)76(131)113-54(22-11-33-106-84(98)99)72(127)110-52(20-9-31-104-82(94)95)71(126)111-53(21-10-32-105-83(96)97)73(128)114-56(29-30-63(93)123)75(130)112-55(23-12-34-107-85(100)101)74(129)115-57(81(136)137)24-13-35-108-86(102)103/h2,5-8,16-19,25-28,40,43,50,52-62,109,121-122H,1,3-4,9-15,20-24,29-39,41-42,92H2,(H2,93,123)(H,110,127)(H,111,126)(H,112,130)(H,113,131)(H,114,128)(H,115,129)(H,116,133)(H,117,134)(H,118,135)(H,119,125)(H,120,132)(H,136,137)(H4,94,95,104)(H4,96,97,105)(H4,98,99,106)(H4,100,101,107)(H4,102,103,108)/t50-,52-,53-,54-,55-,56-,57-,58-,59-,60-,61-,62-/m1/s1

SMILES Code: O=C(O)[C@@H](CCCNC(N)=N)NC([C@@H](CCCNC(N)=N)NC([C@@H](CCC(N)=O)NC([C@@H](CCCNC(N)=N)NC([C@@H](CCCNC(N)=N)NC([C@@H](CCCNC(N)=N)NC([C@@H](CC1CCCCC1)NC([C@@H](CC2=C(F)C(F)=C(F)C(F)=C2F)NC([C@@H](CO)NC([C@@H](CC3=CNC4=C3C=CC=C4)NC([C@@H](CO)NC([C@H](N)CC5=CC=C(C(C6=CC=CC=C6)=O)C=C5)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 1929.065 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Shapiro GI, Tibes R, Gordon MS, Wong BY, Eder JP, Borad MJ, Mendelson DS, Vogelzang NJ, Bastos BR, Weiss GJ, Fernandez C, Sutherland W, Sato H, Pierceall WE, Weaver D, Slough S, Wasserman E, Kufe DW, Von Hoff D, Kawabe T, Sharma S. Phase I studies of CBP501, a G2 checkpoint abrogator, as monotherapy and in combination with cisplatin in patients with advanced solid tumors. Clin Cancer Res. 2011 May 15;17(10):3431-42. Epub 2011 Jan 10. PubMed PMID: 21220472.

2: Al-Shamahi A. Japan Biotech Forum: London 2010. IDrugs. 2010 Nov;13(11):756-8. PubMed PMID: 21046519.

3: Walker K, Padhiar M. AACR-NCI-EORTC--21st International Symposium. Molecular targets and cancer therapeutics--Part 1. IDrugs. 2010 Jan;13(1):7-9. PubMed PMID: 20024838.

4: Tomillero A, Moral MA. Gateways to clinical trials. July-August 2008. Methods Find Exp Clin Pharmacol. 2008 Jul-Aug;30(6):459-95. PubMed PMID: 18850047.

5: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Apr;29(3):231-45. PubMed PMID: 17520107.

6: Sha SK, Sato T, Kobayashi H, Ishigaki M, Yamamoto S, Sato H, Takada A, Nakajyo S, Mochizuki Y, Friedman JM, Cheng FC, Okura T, Kimura R, Kufe DW, Vonhoff DD, Kawabe T. Cell cycle phenotype-based optimization of G2-abrogating peptides yields CBP501 with a unique mechanism of action at the G2 checkpoint. Mol Cancer Ther. 2007 Jan;6(1):147-53. PubMed PMID: 17237275.

7: Koizumi Y, Arai M, Tomoda H, Omura S. Oxaline, a fungal alkaloid, arrests the cell cycle in M phase by inhibition of tubulin polymerization. Biochim Biophys Acta. 2004 Jul 23;1693(1):47-55. PubMed PMID: 15276324.



Additional Information

CBP501 is currently being developed by CanBas Co. Randomized Phase II clinical trials are currently ongoing in two indications, malignant pleural mesothelioma (MPM) and non-small cell lung cancer (NSCLC). Phase I studies have been completed in ovarian cancer. (source: http://www.canbas.co.jp/eng/Pipeline/Pipeline-CBP501.html).