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Chemical Structure : BI-2852
CAS No.: 2375482-51-0
Catalog No.: PC-72332Not For Human Use, Lab Use Only.
BI-2852 (BI 2852) is a potent pan-Ras inhibitor, targets GTP-bound KRAS, binds to KRASG12D with a KD of 740 nM (ITC), inhibits GTP-KRAS G12D binding to effectors like SOS1, CRAF and PI3Kα with an IC50 of 490, 770 and 500 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $258 | In stock | |
| 10 mg | $438 | In stock | |
| 50 mg | $988 | In stock | |
| 100 mg | $1680 | In stock | |
| 1 g | Get quote |
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BI-2852 (BI 2852) is a potent pan-Ras inhibitor, targets GTP-bound KRAS, binds to KRASG12D with a KD of 740 nM (ITC), inhibits GTP-KRAS G12D binding to effectors like SOS1, CRAF and PI3Kα with an IC50 of 490, 770 and 500 nM.
BI-2852 showed pERK(2h) modulation and antiproliferative effects in KRASmut cells (NCI-H358) at 5.8 uM and 6.7 uM, displays an IC50 of 490 nM in a GTP-KRASG12D::SOS1 AlphaScreen (AS) assay leading to low micromolar inhibition of pERK (in H358 cell line).
BI-2852 can serve as an excellent small molecule tool inhibitor of KRAS for testing biological hypotheses in vitro.
| M.Wt | C31H28N6O2 | |
| Formula | 516.605 | |
| Appearance | Solid | |
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1. Kessler D, et al. Proc Natl Acad Sci U S A. 2019 Aug 6;116(32):15823-15829.
2. Tran TH, et al. Proc Natl Acad Sci U S A. 2020 Feb 18;117(7):3363-3364.
3. Kessler D, et al. Future Med Chem. 2020 Nov;12(21):1911-1923.
4. Nomura TK, et al. Cell Chem Biol. 2021 Nov 18;28(11):1581-1589.e6.
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