2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. BI-2865

BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM).

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BI-2865 Chemical Structure

BI-2865 Chemical Structure

CAS No. : 2937327-93-8

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 696 In-stock
Solution
10 mM * 1 mL in DMSO USD 696 In-stock
Solid
1 mg USD 270 In-stock
5 mg USD 680 In-stock
10 mg USD 820 In-stock
25 mg USD 1250 In-stock
50 mg USD 1650 In-stock
100 mg USD 2250 In-stock
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Based on 1 publication(s) in Google Scholar

BI-2865 Related Antibodies

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Description

BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM)[1].

In Vitro

BI-2865 is a derivative with a prolinol substituent and a pyrimidine linker. BI-2865 has direct ionic interaction with E62, and a water-mediated hydrogen bond network with the side chain of R68 and the main chain carbonyl of Q61, as shown in Co-crystal structures of BI-2865 bound to KRAS[1].
BI-2865 (5 days) inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells in the presence of IL-13, with a mean IC50 of roughly 140 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BI-2865 Related Antibodies
Molecular Weight

465.57

Formula

C23H27N7O2S
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

N#CC1=C(N)SC2=C1[C@@](C)(C3=NC(C4=NC(O[C@@H](C)[C@@H]5CCCN5C)=CC=N4)=NO3)CCC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (536.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1479 mL 10.7395 mL 21.4790 mL
5 mM 0.4296 mL 2.1479 mL 4.2958 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1479 mL 10.7395 mL 21.4790 mL 53.6976 mL
5 mM 0.4296 mL 2.1479 mL 4.2958 mL 10.7395 mL
10 mM 0.2148 mL 1.0740 mL 2.1479 mL 5.3698 mL
15 mM 0.1432 mL 0.7160 mL 1.4319 mL 3.5798 mL
20 mM 0.1074 mL 0.5370 mL 1.0740 mL 2.6849 mL
25 mM 0.0859 mL 0.4296 mL 0.8592 mL 2.1479 mL
30 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7899 mL
40 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3424 mL
50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0740 mL
60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8950 mL
80 mM 0.0268 mL 0.1342 mL 0.2685 mL 0.6712 mL
100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5370 mL
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BI-2865 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BI-28652937327-93-8BI2865BI 2865RasCancerKRAS inhibitorBaF3 cellKRAS mutantInhibitorinhibitorinhibit

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