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MedKoo Cat#: 532809 | Name: BI 882370
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Description:

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

BI 882370 is a highly potent and selective RAF inhibitor that binds to the DFG-out (inactive) conformation of the BRAF kinase. BI 882370 inhibits proliferation of human BRAF-mutant melanoma cells with 100× higher potency (1-10 nmol/L) than vemurafenib.

Chemical Structure

BI 882370
BI 882370
CAS#1392429-79-6

Theoretical Analysis

MedKoo Cat#: 532809

Name: BI 882370

CAS#: 1392429-79-6

Chemical Formula: C28H33F2N7O2S

Exact Mass: 569.2385

Molecular Weight: 569.68

Elemental Analysis: C, 59.03; H, 5.84; F, 6.67; N, 17.21; O, 5.62; S, 5.63

Price and Availability

Size Price Availability Quantity
100mg USD 950.00 2 Weeks
200mg USD 1,450.00 2 Weeks
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Related CAS #
No Data
Synonym
BI 882370; BI-882370; BI882370.
IUPAC/Chemical Name
N-(3-(5-((1-ethylpiperidin-4-yl)(methyl)amino)-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl)-2,4-difluorophenyl)propane-1-sulfonamide
InChi Key
GAIOPWBQKZMUNO-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H15FN6O2S2/c1-8-13(25-15(18-2)20-8)12-11(16)7-19-14(22-12)21-9-4-3-5-10(6-9)26(17,23)24/h3-7H,1-2H3,(H,18,20)(H2,17,23,24)(H,19,21,22)
SMILES Code
O=S(C1=CC=CC(NC2=NC=C(F)C(C3=C(C)N=C(NC)S3)=N2)=C1)(N)=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
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
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
BI-882370 is a RAF kinase inhibitor which inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively.
In vitro activity:
High potency of BI 882370 was observed in cellular assays. In human A375 melanoma cells carrying a homozygous BRAFV600E mutation, treatment for 2 hours resulted in a reduction of phospho-MEK1/2 and phospho-ERK1/2 signals as seen in immunoblots, with EC50 values estimated as 0.3 nmol/L and complete suppression observed at 3 nmol/L (Fig. 2A). Treatment for 24 hours suppressed cyclin D1/D2 expression, whereas Kip1/p27 was induced at concentrations of 1 nmol/L or higher, indicating a cell-cycle arrest in the G1 phase. The potency of the compound was also determined in cell-based ELISAs for ERK phosphorylation (Table 2). BI 882370 showed EC50 values of 0.5 and 0.7 nmol/L in A375 and SK-MEL-28 (BRAFV600E) melanoma cells, respectively. Reference: Mol Cancer Ther. 2016 Mar;15(3):354-65. https://mct.aacrjournals.org/content/15/3/354.long
In vivo activity:
Treatment of mice bearing established A375 melanomas (50–100 mm3) with BI 882370 at doses of 6.25 or 12.5 mg/kg twice daily resulted in high efficacy; on day 18, when the control group had to be sacrificed for ethical reasons (median tumor volume, 1,000 mm3), the median TGI was higher than 100%, and partial regressions were observed in subsets of tumors. At 25 mg/kg twice daily, all tumors showed either partial (3/7) or complete (4/7) regression. BI 882370 was well tolerated at all dose levels, as judged by body weight gain and clinical signs. Reference: Mol Cancer Ther. 2016 Mar;15(3):354-65. https://mct.aacrjournals.org/content/15/3/354.long
Solvent mg/mL mM comments
Solubility
DMSO 5.0 8.78
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 569.68 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
Formulation protocol:
1. Waizenegger IC, Baum A, Steurer S, Stadtmüller H, Bader G, Schaaf O, Garin-Chesa P, Schlattl A, Schweifer N, Haslinger C, Colbatzky F, Mousa S, Kalkuhl A, Kraut N, Adolf GR. A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation. Mol Cancer Ther. 2016 Mar;15(3):354-65. doi: 10.1158/1535-7163.MCT-15-0617. Epub 2016 Feb 25. PMID: 26916115.
In vitro protocol:
1. Waizenegger IC, Baum A, Steurer S, Stadtmüller H, Bader G, Schaaf O, Garin-Chesa P, Schlattl A, Schweifer N, Haslinger C, Colbatzky F, Mousa S, Kalkuhl A, Kraut N, Adolf GR. A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation. Mol Cancer Ther. 2016 Mar;15(3):354-65. doi: 10.1158/1535-7163.MCT-15-0617. Epub 2016 Feb 25. PMID: 26916115.
In vivo protocol:
1. Waizenegger IC, Baum A, Steurer S, Stadtmüller H, Bader G, Schaaf O, Garin-Chesa P, Schlattl A, Schweifer N, Haslinger C, Colbatzky F, Mousa S, Kalkuhl A, Kraut N, Adolf GR. A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation. Mol Cancer Ther. 2016 Mar;15(3):354-65. doi: 10.1158/1535-7163.MCT-15-0617. Epub 2016 Feb 25. PMID: 26916115.
1: Waizenegger IC, Baum A, Steurer S, Stadtmüller H, Bader G, Schaaf O, Garin-Chesa P, Schlattl A, Schweifer N, Haslinger C, Colbatzky F, Mousa S, Kalkuhl A, Kraut N, Adolf GR. A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation. Mol Cancer Ther. 2016 Mar;15(3):354-65. doi: 10.1158/1535-7163.MCT-15-0617. Epub 2016 Feb 25. PubMed PMID: 26916115.