2. MAPK/ERK Pathway Apoptosis
  3. Raf Apoptosis
  4. HG6-64-1

HG6-64-1 (HMSL 10017-101-1) is a B-raf kinase modulator.HG6-64-1 modulates B-raf kinase activity, including the V600E mutant form and the drug-resistant gatekeeper mutation T529I. HG6-64-1 is a germinal center kinase inhibitor. HG6-64-1 induces cell cycle arrest and apoptosis. HG6-64-1 can be used for the research of diffuse large B-cell lymphoma (DLBCL).

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

HG6-64-1

HG6-64-1 Chemical Structure

CAS No. : 1315329-43-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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HG6-64-1 Related Antibodies

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Description

HG6-64-1 (HMSL 10017-101-1) is a B-raf kinase modulator.HG6-64-1 modulates B-raf kinase activity, including the V600E mutant form and the drug-resistant gatekeeper mutation T529I. HG6-64-1 is a germinal center kinase inhibitor. HG6-64-1 induces cell cycle arrest and apoptosis. HG6-64-1 can be used for the research of diffuse large B-cell lymphoma (DLBCL)[1][2].

IC50 & Target

B-RafV600E

0.09 μM (IC50, in Ba/F3 cells)

Cellular Effect
Cell Line Type Value Description References
BaF3 IC50
0.01 μM
Compound: 2
Antiproliferative activity against parental mouse BaF3 cells harbouring Bcr/Abl assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
Antiproliferative activity against parental mouse BaF3 cells harbouring Bcr/Abl assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
[PMID: 25075558]
BaF3 IC50
4.018 μM
Compound: 2
Antiproliferative activity against parental mouse BaF3 cells assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
Antiproliferative activity against parental mouse BaF3 cells assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
[PMID: 25075558]
In Vitro

HG6-64-1 (example XI-1) (48 h) inhibits proliferation of B-RAFV600E transformed Ba/F3 cells with an IC50 of 0.09 μM[1].
HG6-64-1 inhibits proliferation of multiple cancer cell lines, with most potent activity against B-RAFV600E transformed lines, including IC50 values as low as 0.09 μM in BRAF/Baf3V600E cells, 0.18 μM in A375 cells, and 0.19 μM in K029 cells[1].
HG6-64-1 inhibits proliferation of Ba/F3 cells expressing the drug-resistant B-RAFV600E/T529I double mutation with an approximate IC50 of 400 nM[1].
HG6-64-1 binds to and inhibits a broad range of kinases in HL60 cell lysates, with the highest inhibition observed for LYN, CSK, HPK1, ABL1/2, and TAO1/3[1].
HG6-64-1 leads to cell cycle arrest and the induction of apoptosis in DLBCL cell lines and primary DLBCL tumors. G452, a DLBCL cell line minimally expressing GCK, is not affected by HG6-64-1[2].

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

HG6-64-1 Related Antibodies
In Vivo

In vivo treatment with HG6-64-1, via intratumoral and intraperitoneal injections, significantly decreased the tumor growth rate resulting in a significantly extended lifespan of DLBCL xenograft mouse models[2].

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

577.64

Formula

C32H34F3N5O2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(NC1=CC=C(CN2CCN(CC)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(/C=C/C4=CN=C(NC=C5)C5=C4OC)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 75 mg/mL (129.84 mM; ultrasonic and warming and heat to 60°C; 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 1.7312 mL 8.6559 mL 17.3118 mL
5 mM 0.3462 mL 1.7312 mL 3.4624 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 (protect from light, 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 3 mg/mL (5.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 3 mg/mL (5.19 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 3 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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 (protect from light, 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 1.7312 mL 8.6559 mL 17.3118 mL 43.2796 mL
5 mM 0.3462 mL 1.7312 mL 3.4624 mL 8.6559 mL
10 mM 0.1731 mL 0.8656 mL 1.7312 mL 4.3280 mL
15 mM 0.1154 mL 0.5771 mL 1.1541 mL 2.8853 mL
20 mM 0.0866 mL 0.4328 mL 0.8656 mL 2.1640 mL
25 mM 0.0692 mL 0.3462 mL 0.6925 mL 1.7312 mL
30 mM 0.0577 mL 0.2885 mL 0.5771 mL 1.4427 mL
40 mM 0.0433 mL 0.2164 mL 0.4328 mL 1.0820 mL
50 mM 0.0346 mL 0.1731 mL 0.3462 mL 0.8656 mL
60 mM 0.0289 mL 0.1443 mL 0.2885 mL 0.7213 mL
80 mM 0.0216 mL 0.1082 mL 0.2164 mL 0.5410 mL
100 mM 0.0173 mL 0.0866 mL 0.1731 mL 0.4328 mL
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HG6-64-1 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:

HG6-64-11315329-43-1HMSL 10017-101-1RafApoptosisRaf kinasesCSKBa/F3 cellsHL60 cell lysatesLYNA375 cellsT529I mutationcancerB-raf kinaseV600E mutantK029 cellsInhibitorinhibitorinhibit

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