BRSD-212
BRSD-212 is an orally active KRAS G12V/G12D inhibitor. BRSD-212 binds the switch-II pocket and inhibits GDP- and GMPPNP-bound mutant KRAS, with IC50 <0.2 nM for both variants. BRSD-212 inhibits ERK phosphorylation in KRAS-mutant tumor cell lines. BRSD-212 induces tumor regression and inhibits tumor growth in xenograft models. BRSD-212 is well tolerated in murine tumor models with no body weight change. BRSD-212 can be used for the research of cancer.
For research use only. We do not sell to patients.
- Formula: C37H42F2N6O4
- Molecular Weight:672.76
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
KRas G12V |
KRas G12D |
ERK |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C.B-17/IcrHsd-PrkdcscidLystbg-J (female)[1]
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Dosage:1 mg/kg; 3 mg/kg
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Administration:p.o.
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Result:Achieved 41% tumor regression at 3 mg/kg by day 4.
No body weight change was detected.
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Animal Model:Crl:NU(NCr)-Foxn1nu-homozygous nude (female)[1]
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Dosage:30 mg/kg
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Administration:p.o.
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Result:Demonstrated equivalent efficacy to the comparator at 30 mg/kg in the SW1990 xenograft model.
No body weight change was detected.
- Kinase activity and phosphorylation assays
- Western Blot
- Patient-Derived Xenograft (PDX)
- Patient-Derived Orthotopic Xenograft (PDOX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Molecular Weight 672.76
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Formula C37H42F2N6O4
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SMILES
C[C@@]12CCCN(C3=NC(OC[C@H]4C[C@@H](C)N(C)[C@H]5[C@@H]4CC5)=NC6=C(C(C7=C8C(C=CC(F)=C8CCCOC(N2)=O)=CC(O)=C7)=NC=C36)F)C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BRSD-212 Related Classifications
HY-189619 Related Classifications
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