1. MAPK/ERK Pathway
  2. Raf
  3. RAF709

RAF709 

Cat. No.: HY-100510 Purity: 98.87%
COA Handling Instructions

RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively. Antitumor efficacy.

For research use only. We do not sell to patients.

RAF709 Chemical Structure

RAF709 Chemical Structure

CAS No. : 1628838-42-5

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 118 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 118 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 99 In-stock
Estimated Time of Arrival: December 31
10 mg USD 165 In-stock
Estimated Time of Arrival: December 31
25 mg USD 330 In-stock
Estimated Time of Arrival: December 31
50 mg USD 539 In-stock
Estimated Time of Arrival: December 31
100 mg USD 869 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

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  • Purity & Documentation

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Description

RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively[1]. Antitumor efficacy[1].

IC50 & Target

CRAF

0.5 nM (IC50)

Braf

0.4 nM (IC50)

In Vitro

RAF709 stabilizes BRAF-CRAF dimers with an EC50 of 0.8 μM. In cellular assays, the dose-response of pMEK and pERK are measured in Calu-6 cells with EC50=0.02 and 0.1 μM with minimal paradoxical activation and inhibition of proliferation with EC50=0.95 μM[1].

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

In Vivo

RAF709 proves to be soluble, kinase selective, and efficacious in a KRAS mutant xenograft model. RAF709 shows dose-proportional increases in plasma exposure and a corresponding dosedependent inhibition of pERK in Calu-6 tumors. Treatment with RAF709 results in dose-dependent antitumor activity with 10 mg/kg being subefficacious (%T/C=92%), 30 mg/kg results in measurable antitumor activity (%T/C=46%), and 200 mg/kg results in mean tumor regression of 92%, while the same high dose is not efficacious in the PC3, KRAS WT model[1].

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

Molecular Weight

542.55

Formula

C28H29F3N4O4

CAS No.
SMILES

O=C(NC1=CN=C(C)C(C2=CC(N3CCOCC3)=C(OC4CCOCC4)N=C2)=C1)C5=CC=CC(C(F)(F)F)=C5

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 : 100 mg/mL (184.31 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8431 mL 9.2157 mL 18.4315 mL
5 mM 0.3686 mL 1.8431 mL 3.6863 mL
10 mM 0.1843 mL 0.9216 mL 1.8431 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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Product Name:
RAF709
Cat. No.:
HY-100510
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