BI-D1870
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MedKoo CAT#: 500405

CAS#: 501437-28-1

Description: BI-D1870 is a potent and specific RSK inhibitor (the p90 ribosomal S6 kinase), which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro with an IC50 of 10–30 nM. BI-D1870 exhibited a dose-responsive antiproliferative effect on OSCC cells with relative sparing of normal human oral keratinocytes. The compound inhibited the downstream RSK target YB-1 and caused apoptosis. In addition, BI-D1870 also induced G2/M arrest by modulating the expression of p21 and other cell cycle regulators. BI-D1870 may be of useful in oral squamous cell carcinoma therapy.


Chemical Structure

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BI-D1870
CAS# 501437-28-1

Theoretical Analysis

MedKoo Cat#: 500405
Name: BI-D1870
CAS#: 501437-28-1
Chemical Formula: C19H23F2N5O2
Exact Mass: 391.18198
Molecular Weight: 391.41
Elemental Analysis: C, 58.30; H, 5.92; F, 9.71; N, 17.89; O, 8.18

Size Price Shipping out time Quantity
10mg USD 150 2 Weeks
25mg USD 250 2 Weeks
50mg USD 450 2 Weeks
100mg USD 750 2 Weeks
200mg USD 1250 2 Weeks
500mg USD 2150 2 Weeks
1g USD 3150 2 Weeks
2g USD 5450 2 Weeks
Inquire bulk and customized quantity

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

BI-D1870 is in stock

Synonym: BID1870; BI D1870; BI-D1870.

IUPAC/Chemical Name: 2-((3,5-difluoro-4-hydroxyphenyl)amino)-8-isopentyl-5,7-dimethyl-7,8-dihydropteridin-6(5H)-one.

InChi Key: DTEKTGDVSARYDS-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H23F2N5O2/c1-10(2)5-6-26-11(3)18(28)25(4)15-9-22-19(24-17(15)26)23-12-7-13(20)16(27)14(21)8-12/h7-11,27H,5-6H2,1-4H3,(H,22,23,24)

SMILES Code: O=C1N(C)C2=CN=C(NC3=CC(F)=C(O)C(F)=C3)N=C2N(CCC(C)C)C1C

Appearance:
Pale orange to brown 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:
>2 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

Certificate of Analysis:

Safety Data Sheet (SDS):

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 391.41 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: Edgar AJ, Trost M, Watts C, Zaru R. A combination of SILAC and nucleotide acyl phosphate labelling reveals unexpected targets of the Rsk inhibitor BI-D1870. Biosci Rep. 2013 Dec 17. [Epub ahead of print] PubMed PMID: 24341623; PubMed Central PMCID: PMC3908613.

2: Chiu CF, Bai LY, Kapuriya N, Peng SY, Wu CY, Sargeant AM, Chen MY, Weng JR. Antitumor effects of BI-D1870 on human oral squamous cell carcinoma. Cancer Chemother Pharmacol. 2014 Feb;73(2):237-47. doi: 10.1007/s00280-013-2349-9. Epub 2013 Nov 16. PubMed PMID: 24241211.

3: Neise D, Sohn D, Stefanski A, Goto H, Inagaki M, Wesselborg S, Budach W, Stühler K, Jänicke RU. The p90 ribosomal S6 kinase (RSK) inhibitor BI-D1870 prevents gamma irradiation-induced apoptosis and mediates senescence via RSK- and p53-independent accumulation of p21WAF1/CIP1. Cell Death Dis. 2013 Oct 17;4:e859. doi: 10.1038/cddis.2013.386. PubMed PMID: 24136223; PubMed Central PMCID: PMC3920941.

4: Sapkota GP, Cummings L, Newell FS, Armstrong C, Bain J, Frodin M, Grauert M, Hoffmann M, Schnapp G, Steegmaier M, Cohen P, Alessi DR. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem J. 2007 Jan 1;401(1):29-38. PubMed PMID: 17040210; PubMed Central PMCID: PMC1698666.



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