1. GPCR/G Protein
  2. Ras

Pan-RAS-IN-1 

Cat. No.: HY-101295 Purity: >98.0%
Handling Instructions

Pan-RAS-IN-1 is a pan-Ras inhibitor that disrupts the interaction of Ras proteins and their effectors.

For research use only. We do not sell to patients.
Pan-RAS-IN-1 Chemical Structure

Pan-RAS-IN-1 Chemical Structure

CAS No. : 1835283-94-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 663 In-stock
1 mg USD 180 In-stock
5 mg USD 420 In-stock
10 mg USD 720 In-stock
25 mg USD 1440 In-stock
50 mg USD 2340 In-stock
100 mg USD 4080 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Pan-RAS-IN-1 is a pan-Ras inhibitor that disrupts the interaction of Ras proteins and their effectors.

In Vitro

Pan-RAS-IN-1 binds to KRasG12D-GppNHp with an affinity less than 20 μM. Pan-RAS-IN-1 binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins. The potency of pan-RAS-IN-1 correlates with the degree of dependency on the mutated isoform over a 5-fold concentration range. At some concentrations, pan-RAS-IN-1 is cytostatic, possibly due to pan-RAS inhibition. Pan-RAS-IN-1 is evaluated in primary T cell acute lymphoblastic leukemia (T-ALL) cells. Selective lethality is observed, with mutant NRAS cells retaining only 20%-40% viability after 5 μM treatment[1].

In Vivo

Pan-RAS-IN-1 administration results in inhibition of tumor growth over 15 days of treatment. Pan-RAS-IN-1-treated mice exhibits decreased tumor pERK levels compared with vehicle treated mice. A modest increase in cleaved caspase-3 is also observed, showing that in this model, pan-RAS-IN-1 has the capacity to induce caspase activation[1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.3934 mL 6.9672 mL 13.9344 mL
5 mM 0.2787 mL 1.3934 mL 2.7869 mL
10 mM 0.1393 mL 0.6967 mL 1.3934 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

For 384-well cancer cell viability assays, cells are trypsinized, counted, and seeded into 384-well plates at 1,000 cells/well. After 16 hr, pan-RAS-IN-1 (from 10 mM stocks in DMSO) are arrayed in an 8-point or 16-point dilution series in 384-well polypropylene plates. Compound solutions are transferred at a 1:5 dilution into the assay plates. After 48 hr, a 50% Alamar blue solution is added to a final concentration of 10% Alamar blue. After 6 hr of incubation, fluorescence intensity is determined at 535 and 590 nm[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Mice tumor Xenograft are dosed with 180 mg/kg pan-RAS-IN-1 orally (12 mg/mL, 10% DMSO, pH 4), vehicle orally, or by a combination of i.p. and i.v. injections at 30 mg/kg (4 mg/mL, 5% DMSO in HBSS at pH 4). Over 14 d, mice receive a total of 10 doses of pan-RAS-IN-1 or vehicle orally, or six i.p. injections and 4 i.v. injections. Tumor size is measured by electronic caliper every 2 d and calculated[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

717.65

Formula

C₃₆H₄₁Cl₂F₃N₆O₂

CAS No.

1835283-94-7

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: >98.0%

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Product Name:
Pan-RAS-IN-1
Cat. No.:
HY-101295
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