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Cat. No.: 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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

화학식: C₃₇H₄₂F₂N₆O₄
분자량:672.76

보관:

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

BRSD-212 Chemical Structure

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

KRas G12V

KRas G12D

ERK

All Ras Isoforms :

All ERK Isoforms :

In Vitro

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.

In Vivo

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 :

Chemical Information

분자량 672.76
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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

견적 받기

Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

BRSD-212

All Ras Isoforms

All ERK Isoforms