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  4. (R)-BI-2852

(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

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(R)-BI-2852 Chemical Structure

(R)-BI-2852 Chemical Structure

CAS No. : 2375482-49-6

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1 mg USD 120 In-stock
5 mg USD 230 In-stock
10 mg USD 360 In-stock
50 mg USD 1100 In-stock
100 mg USD 1750 In-stock
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Based on 1 publication(s) in Google Scholar

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(R)-BI-2852 Related Antibodies

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Description

(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

Molecular Weight

516.59

Formula

C31H28N6O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

OC(C=C1)=CC([C@H](C2=C(CNCC3=CC4=C(C=CN4CC5=CN(C)C=N5)C=C3)NC6=CC=CC=C62)N7)=C1C7=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 55 mg/mL (106.47 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 1.9358 mL 9.6789 mL 19.3577 mL
5 mM 0.3872 mL 1.9358 mL 3.8715 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 97.32% ee.: 100.00%

COA (263 KB) HNMR (314 KB) NP-HPLC (271 KB) LCMS (142 KB)

Handling Instructions (2659 KB)
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 (stored under nitrogen). 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 1.9358 mL 9.6789 mL 19.3577 mL 48.3943 mL
5 mM 0.3872 mL 1.9358 mL 3.8715 mL 9.6789 mL
10 mM 0.1936 mL 0.9679 mL 1.9358 mL 4.8394 mL
15 mM 0.1291 mL 0.6453 mL 1.2905 mL 3.2263 mL
20 mM 0.0968 mL 0.4839 mL 0.9679 mL 2.4197 mL
25 mM 0.0774 mL 0.3872 mL 0.7743 mL 1.9358 mL
30 mM 0.0645 mL 0.3226 mL 0.6453 mL 1.6131 mL
40 mM 0.0484 mL 0.2420 mL 0.4839 mL 1.2099 mL
50 mM 0.0387 mL 0.1936 mL 0.3872 mL 0.9679 mL
60 mM 0.0323 mL 0.1613 mL 0.3226 mL 0.8066 mL
80 mM 0.0242 mL 0.1210 mL 0.2420 mL 0.6049 mL
100 mM 0.0194 mL 0.0968 mL 0.1936 mL 0.4839 mL
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(R)-BI-2852 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:

(R)-BI-28522375482-49-6OthersInhibitorinhibitorinhibit

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