SB-218078
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406348

CAS#: 135897-06-2

Description: SB-218078 is a potent and selective indolocarbazole chk1 inhibitor.


Chemical Structure

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SB-218078
CAS# 135897-06-2

Theoretical Analysis

MedKoo Cat#: 406348
Name: SB-218078
CAS#: 135897-06-2
Chemical Formula: C24H15N3O3
Exact Mass: 393.11
Molecular Weight: 393.3942
Elemental Analysis: C, 73.27; H, 3.84; N, 10.68; O, 12.20

Size Price Shipping out time Quantity
1mg USD 295 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-02-26. Prices are subject to change without notice.

SB-218078, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Synonym: SB218078; SB218078; SB218078.

IUPAC/Chemical Name: (5R,8S)-7,8-dihydro-5H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-13,15(6H,14H)-dione

InChi Key: OTPNDVKVEAIXTI-IYBDPMFKSA-N

InChi Code: InChI=1S/C24H15N3O3/c28-23-19-17-11-5-1-3-7-13(11)26-15-9-10-16(30-15)27-14-8-4-2-6-12(14)18(22(27)21(17)26)20(19)24(29)25-23/h1-8,15-16H,9-10H2,(H,25,28,29)/t15-,16+

SMILES Code: O=C1NC(C(C2=C3N([C@@]4([H])CC[C@]5([H])O4)C6=CC=CC=C62)=C1C7=C3N5C8=CC=CC=C78)=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:
0 – 4 C for short term (weeks to 1 month) or -20 C for long terms (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly.

Drug Formulation:
Stock solution storage:

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

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 393.3942 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.

Select a batch to recalculate based on the batch molecular weight:
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: Jennings-Gee J, Pardee TS, Gmeiner WH. Replication-dependent irreversible topoisomerase 1 poisoning is responsible for FdUMP[10] anti-leukemic activity. Exp Hematol. 2013 Feb;41(2):180-188.e4. doi: 10.1016/j.exphem.2012.10.007. Epub 2012 Oct 17. PubMed PMID: 23085462; PubMed Central PMCID: PMC3660094.

2: Park JH, Kim WS, Kim JY, Park MH, Nam JH, Yun CW, Kwon YG, Jo I. Chk1 and Hsp90 cooperatively regulate phosphorylation of endothelial nitric oxide synthase at serine 1179. Free Radic Biol Med. 2011 Dec 15;51(12):2217-26. doi: 10.1016/j.freeradbiomed.2011.09.021. Epub 2011 Sep 25. PubMed PMID: 22001744.

3: Fishler T, Li YY, Wang RH, Kim HS, Sengupta K, Vassilopoulos A, Lahusen T, Xu X, Lee MH, Liu Q, Elledge SJ, Ried T, Deng CX. Genetic instability and mammary tumor formation in mice carrying mammary-specific disruption of Chk1 and p53. Oncogene. 2010 Jul 15;29(28):4007-17. doi: 10.1038/onc.2010.163. Epub 2010 May 17. PubMed PMID: 20473325.

4: Azorsa DO, Gonzales IM, Basu GD, Choudhary A, Arora S, Bisanz KM, Kiefer JA, Henderson MC, Trent JM, Von Hoff DD, Mousses S. Synthetic lethal RNAi screening identifies sensitizing targets for gemcitabine therapy in pancreatic cancer. J Transl Med. 2009 Jun 11;7:43. doi: 10.1186/1479-5876-7-43. PubMed PMID: 19519883; PubMed Central PMCID: PMC2702280.

5: Robles AI, Wright MH, Gandhi B, Feis SS, Hanigan CL, Wiestner A, Varticovski L. Schedule-dependent synergy between the heat shock protein 90 inhibitor 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin and doxorubicin restores apoptosis to p53-mutant lymphoma cell lines. Clin Cancer Res. 2006 Nov 1;12(21):6547-56. PubMed PMID: 17085670.

6: Chen JS, Lin SY, Tso WL, Yeh GC, Lee WS, Tseng H, Chen LC, Ho YS. Checkpoint kinase 1-mediated phosphorylation of Cdc25C and bad proteins are involved in antitumor effects of loratadine-induced G2/M phase cell-cycle arrest and apoptosis. Mol Carcinog. 2006 Jul;45(7):461-78. PubMed PMID: 16649252.

7: Kawabe T. G2 checkpoint abrogators as anticancer drugs. Mol Cancer Ther. 2004 Apr;3(4):513-9. Review. PubMed PMID: 15078995.

8: Zhao B, Bower MJ, McDevitt PJ, Zhao H, Davis ST, Johanson KO, Green SM, Concha NO, Zhou BB. Structural basis for Chk1 inhibition by UCN-01. J Biol Chem. 2002 Nov 29;277(48):46609-15. Epub 2002 Sep 19. PubMed PMID: 12244092.

9: Jackson JR, Gilmartin A, Imburgia C, Winkler JD, Marshall LA, Roshak A. An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage. Cancer Res. 2000 Feb 1;60(3):566-72. PubMed PMID: 10676638.



Additional Information