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United States

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製品番号: HY-189619

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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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₃₇H₄₂F₂N₆O₄
分子量:672.76

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

BRSD-212 構造式

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
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生物活性

製品説明

IC₅₀ & Target

^[1]

KRas G12V

KRas G12D

ERK

Ras アイソフォーム固有の製品をすべて表示 :

ERK アイソフォーム固有の製品をすべて表示 :

体外実験

Anti-cancerOthers

Anti-cancer

BRSD-212 (compound 12) inhibits pERK in RKN and SW1990 cells with IC₅₀ values of 2.0 nM and 0.6 nM, respectively^[1].

Others

BRSD-212 exhibits sub-nanomolar biochemical activity against GDP-bound and GMPPNP-bound KRAS^G12V and KRAS^G12D, with IC₅₀ values <0.2 nM^[1].
BRSD-212 exhibits high MDCK permeability of 22.9 × 10⁻⁶ cm/s^[1].

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

体内実験

Anti-cancer

BRSD-212 (compound 12) (1-3 mg/kg; p.o.; up to day 4) produces 41% tumor regression in the RKN xenograft model^[1].
BRSD-212 (30 mg/kg; p.o.) shows effects comparable to the control drug in the SW1990 xenograft model^[1].

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

Animal Model:

C.B-17/IcrHsd-PrkdcscidLystbg-J (female)^[1]
Dosage:

1 mg/kg; 3 mg/kg
Administration:

p.o.
Result:

Achieved 41% tumor regression at 3 mg/kg by day 4.
No body weight change was detected.

Animal Model:

Crl:NU(NCr)-Foxn1nu-homozygous nude (female)^[1]
Dosage:

30 mg/kg
Administration:

p.o.
Result:

Demonstrated equivalent efficacy to the comparator at 30 mg/kg in the SW1990 xenograft model.
No body weight change was detected.

Related Protocols :

化学情報

分子量 672.76
分子式 C₃₇H₄₂F₂N₆O₄
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Phillips DP, et al. Lead Optimization of Multimutant KRAS Switch-II Pocket Macrocyclic Inhibitors via Isosteric Replacement to Improve ADME and Oral Exposure. Journal of medicinal chemistry. 2026 Sep 10;69(17):20698-20718.

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

お問い合わせ

Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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BRSD-212

Ras アイソフォーム固有の製品をすべて表示

ERK アイソフォーム固有の製品をすべて表示