BI-882370
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $1450 | Check With Us |
500mg | $2150 | Check With Us |
1g | $3225 | Check With Us |
Cat #: V4710 CAS #: 1392429-79-6 Purity ≥ 98%
Description: BI-882370 (BI 882370), structurally similar to vermurafenib, is a novel, highly potent and selective BRAF inhibitor with anticancer activity.
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Molecular Weight (MW) | 569.67 |
---|---|
Molecular Formula | C28H33F2N7O2S |
CAS No. | 1392429-79-6 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
SMILES Code | O=S(C1=CC=CC(NC2=NC=C(F)C(C3=C(C)N=C(NC)S3)=N2)=C1)(N)=O |
Synonyms | BI 882370; BI-882370; BI882370 |
Protocol | In Vitro | BI 882370 (0.1-100 nM, 0.1-3000 nM; 24 hours) suppresses cyclin D1/D2 expression, induces Kip1/p27 expression at concentrations of 1 nM or higher in BRAFV600E-mutant A375 cells, expression of cyclins D1/D2 or Kip1/p27 is not affected in WT BRO cells. BI 882370 (0.1-100 nM, 0.1-3000 nM; 2 hours) results in a reduction of p-MEK1/2, p-ERK1/2 and cyclin D1/D2 expression in BRAFV600E-mutant A375 cells; induces phosphorylation of MEK1/2 and enhanced phosphorylation of ERK1/2 in WT BRO cells (3-300 nM). BI-882370 (0.9-6000 nM; 3 days) inhibits the BRAF-mutant human melanoma and colorectal cancer cells proliferation with a EC50 range of 1-10 nM. |
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In Vivo | BI-882370 (deliver orally; 60 mg/kg; once daily; 2 weeks) indicates lack of toxicity in terms of clinical chemistry, hematology, pathology, and toxicogenomics in rats. BI-882370 (deliver orally; 25 mg/kg; twice daily; 40 days) developes resistance within 3 weeks, but resistance is not observed during 5 weeks of second-line therapy in combination with trametinib. BI-882370 (deliver orally; 25 mg/kg, 50 mg/kg; twice daily; 2 weeks) is efficacious in multiple mouse models of BRAF-mutant melanomas and colorectal carcinomas, shows superior efficacy compared with Vemurafenib, Dabrafenib, or Trametinib. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.7554 mL | 8.7770 mL | 17.5540 mL | 35.1080 mL |
5mM | 0.3511 mL | 1.7554 mL | 3.5108 mL | 7.0216 mL |
10mM | 0.1755 mL | 0.8777 mL | 1.7554 mL | 3.5108 mL |
20mM | 0.0878 mL | 0.4389 mL | 0.8777 mL | 1.7554 mL |
The molarity calculator equation
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Method for preparing in vivo formulation:
Take
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PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
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